Substituted indazole arthropodicides

ABSTRACT

Indazole arthropodicides, compositions containing them and a method for controlling arthropods employing these indazoles as the active ingredient. The indazoles have the following general formula wherein Q, X, Y, R 1  and m are as defined in the text: ##STR1##

CROSS-REFERENCE TO RELATED PATENT APPLICATION

This application is a continuation-in-part via the PCT of application Ser. No. 07/249,883 filed on 27 September 1988 and application Ser. No. 07/247,690, filed on 22 September 1988, both now abandoned.

BACKGROUND OF THE INVENTION

U.S. Pat. No. 4,070,365 discloses insecticidal compounds of the formula ##STR2## wherein R₂ and R₃ are independently alkyl, cycloalkyl, pyridyl or thienyl optionally substituted with halogen, alkyl or nitro, or a phenyl group optionally substituted with 1 or 2 substituents selected from halogen, alkyl, haloalkyl, cycloalkyl alkylthio, alkoxy, mono or dialkylamino, nitro, phenyl optionally substituted with halogen or cyano;

Y is halogen, NO₂, alkyl, haloalkyl, cycloalkyl, alkylthio, alkoxy, dialkylamino, alkylsulfonyl, acyl, acylamino, cyano, or a phenyl optionally substituted with halogen; and X is O or S.

U.S. Pat. No. 4,663,341 discloses insecticidal compounds of the formula ##STR3## wherein A is unsubstituted or substituted phenyl;

B is unsubstituted or substituted phenyl;

U is O, S or NR;

Y is alkyl, carbonyl or phenyl each of which may be optionally substituted; and

Z is an organic radical other than hydrogen.

Vaughan, J. Org. Chem., 20 (1955), pages 1619 to 1626, discloses 1,5-diphenyl-2-pyrazoline-3-carboxamide. No utility is given for the disclosed compound which, in any event, does not suggest a compound of the instant invention.

Harhash et al., J. Heterocyclic Chem., 21 (1984), at page 1013, discloses the preparation of five pyrazoline compounds, none of which is disclosed in the instant application. No utility is given for any of said compounds: ##STR4## where R/Ar are C₆ H₅ /C₆ H₅ ; CO₂ C₂ H₅ /C₆ H₅ ; C(O)NHC₆ H₅ /C₆ H₅ ; CH═CHC₆ H₅ /C₆ H₅ ; and CH₃ /4--NO₂ --C₆ H₄.

WO 88/900910 disclosed insecticidal pyrazolines such as compounds of the formula: ##STR5##

WO 88/302995 discloses insecticidal pyrazolines such as compounds of the formula; ##STR6## wherein, Q is (R₂)_(n) ##STR7## A is 1, 2 or 3-atom bridge having 0 to 3 carbon atoms and 0 to 1 oxygen atom, NR₆ group, or S(O)q group, wherein each carbon individually can be substituted with 1 to 2 substituents selected from 1 to 2 halogen, C.sub. to C₆ alkyl, C₂ to C₄ alkoxycarbonyl or phenyl optionally substituted with 1 to 3 substituents selected from W and one of the carbon atoms can be C(O) or C(S).

EP-A-153,127 discloses insecticidal compounds of the formula ##STR8## wherein A is unsubstituted or substituted phenyl;

B is unsubstituted or substituted phenyl;

U is O, S or NR;

Y is alkyl, carbonyl or a phenyl group; and

Z is cycloalkyl, or a phenyl group.

This application is a cognate of applications bearing U.S. Ser. Nos. 07/249,883 and 07/247,690.

SUMMARY OF THE INVENTION

This invention pertains to the following compounds including all of their geometric and stereoisomers, agriculturally suitable salts thereof, agricultural compositions containing them and their use as arthropodicides: ##STR9## wherein: Q is ##STR10## G is O or S; A is a 0, 1 or 2-atom bridge comprising 0 to 2 carbon atoms, 0 to 1 oxygen atoms, 0 to 1 S(O)_(q) groups or 0 to 1 NR₆ groups wherein each carbon atom is optionally substituted with 1 to 2 substituents selected from R_(a) ;

B is H, C₁ to C₆ alkyl, C₃ to C₆ cycloalkyl optionally substituted with 1 to 2 halogens or 1 to 2 CH₃, C₄ to C₁ to C₆ haloalkyl, C₂ to C₆ alkenyl, C₂ to C₆ alkynyl, C₂ to C₆ alkoxyalkyl, C₂ to C₆ cyanoalkyl, C₃ to C₈ alkoxycarbonylalkyl, CO₂ R₃, C(O)R₃, C(O)NR₃ R₄, C(S)NR₃ R₄, C(S)R₃, C(S)SR₃, phenyl, phenyl substituted with (R₅)p, benzyl, benzyl substituted with 1to 3 substituents independently selected from W, or OR₇ when Q is Q₁ to Q₇ ;

W is halogen, CN, NO₂, C₁ to C₂ alkyl, C₁ to C₂ haloalkyl, C₁ to C₂ alkoxy, C₁ to C₂ haloalkoxy, C₁ to C₂ alkylthio, C₁ to C₂ haloalkylthio, C₁ to C₂ alkylsulfonyl or C₁ to C₂ haloalkylsulfonyl;

R₁, R₂ and R₅ are independently selected from R₃, halogen, CN, N₃, SCN, NO₂, OR₃, SR₃, SOR₃, SO₂ R₃, OC(O)R₃, OSO₂ R₃, CO₂ R₃, C(O)R₃, C(O)NR₃ R₄, SO₂ NR₃ R₄, NR₃ R₄, NR₄ C(O)R₃, OC(O)NHR₃, NR₄ C(O)NHR₃ and NR₄ SO₂ R₃, or when m, n or p is 2, R₁, R₂ or R₅ can be --OCH₂ O--, --OCH₂ CH₂ O--, or --CH₂ CH₂ O--, each of which can be substituted with 1 to 4 halogen atoms or 1 to 2 methyl groups;

R₃ is H, C₁ to C₆ alkyl, C₁ to C₆ haloalkyl, C₂ to C₆ alkenyl, C₂ to C₆ haloalkenyl, C₂ to C₆ alkynyl, C₂ to C₆ haloalkynyl, C₂ to C₆ alkoxyalkyl, C₂ to C₆ alkylthioalkyl, C₁ to C₆ nitroalkyl, C₂ to C₆ cyanoalkyl, C₃ to C₈ alkoxycarbonylalkyl, C₃ to C₆ cycloalkyl, C₃ to C₆ halocycloalkyl, phenyl, benzyl, or phenyl or benzyl substituted with 1 to 3 substituents independently selected from W;

R₄ is H, C₁ to C₄ alkyl or R₃ and R₄ can be taken together as (CH₂)₄, (CH₂)₅ or (CH₂ CH₂ OCH₂ CH₂);

R₆ is H, C₁ to C₄ alkyl, C₁ to C₄ haloalkyl, C₂ to C₄ alkenyl, C₂ to C₄ haloalkenyl, C₂ to C₄ alkynyl, phenyl optionally substituted with W;

R₇ is H, C₁ to C₄ alkyl, C₂ to C₄ alkenyl, C₂ to C₄ alkynyl, C₂ to C₄ alkylcarbonyl, C₂ to C₄ alkoxycarbonyl;

R_(a) is independently selected from H, C₁ to C₆ alkyl, C₂ to C₄ alkoxycarbonyl and phenyl optionally substituted with 1 to 3 substituents independently selected from W;

x is O or S;

n is 1 to 2;

m is 1 to 3;

p is 1 to 3;

q is 0 to 2;

Y is H, C₁ to C₆ alkyl, C₂ to C₆ alkoxyalkyl, CHO, C₂ to C₆ alkylcarbonyl, C₂ to C₆ alkoxycarbonyl, C₂ to C₆ haloalkylcarbonyl, C₁ to C₆ alkylthio, C₁ to C₆ haloalkylthio, phenylthio, phenylthio substituted with 1 to 3substituents independently selected from W, or S-J;

J is ##STR11## R₈ and R₁₂ are independently selected from C₁ to C₆ alkyl, C₁ to C₆ haloalkyl, C₃ to C₆ cycloalkyl, C₄ to C₇ cycloalkylalkyl, phenyl optionally substituted with 1 to 2 substituents independently selected from W, benzyl optionally substituted with 1 to 2 substituents independently selected from W, C₂ to C₆ cyanoalkyl, C₂ to C₆ alkoxyalkyl, C₃ to C₈ alkoxycarbonylalkyl and C₄ to C₈ dialkylaminocarbonylalkyl, or R₈ and R₁₂ can be taken together as (CH₂)₄, (CH₂)₅ or (CH₂)₂ O(CH₂)₂ ;

R₉ is F, C₁ to C₂₂ alkyl, C₁ to C₆ haloalkyl, C₁ to C₂₂ alkoxy, C₂ or C₈ dialkylamino, piperidinyl, pyrollidinyl, morpholino, C₁ to C₄ haloalkoxy, C₁ to C₄ alkoxy substituted with cyano, nitro, C₂ to C₄ alkoxy, C₄ to C₈ alkoxyalkoxy, C₁ to C₂ alkylthio, C₂ to C₃ alkoxycarbonyl, C₃ to C₅ dialkylaminocarbonyl or phenyl, or R₉ is phenyl optionally substituted with 1 to 2 substituents independently selected from W, or phenoxy optionally substituted with 1 to 2 substituents independently selected from W;

R₁₀ and R₁₁ are independently selected from C₁ to C₄ alkyl, C₂ to C₄ haloalkyl and phenyl optionally substituted with 1 to 2 substituents independently selected from W, or R₁₀ and R₁₁ can be taken together as (CH₂)₂, (CH₂)₃ or CH₂ C(CH₃)₂ CH₂ ;

t is 0 to 2; and

Y₁ is O or S.

In the above definitions, the term "alkyl", used either alone or in compound words such as "alkylthio" or "haloalkyl", denotes straight chain or branched alkyl such as methyl, ethyl, n-propyl, isopropyl or the different butyl, pentyl, hexyl isomers.

Alkoxy denotes straight chain or branched alkenes such as vinyl, 1-propenyl, 2-propenyl, 3-propenyl and the different butenyl pentenyl and hexenyl isomers.

Alkynyl denotes straight chain or branched alkynes such as ethynyl, 1-propynyl, 2-propynyl and the different butynyl, pentynyl and hexynyl isomers.

Alkylthio denotes methylthio, ethylthio and the different propylthio and butylthio isomers.

Alkylsulfinyl, alkylsulfonyl, alkylamino, and the like, are defined analogously to the above examples.

Cycloalkyl denotes cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl.

The term "halogen", either alone or in compound words such as "haloalkyl", denotes fluorine, chlorine, bromine or iodine. When used in compound words such as "haloalkyl" said alkyl may be partially or fully substituted with halogen atoms, which may be the same or different. Examples of haloalkyl include CH₂ CH₂ F, CF₂ CF₃ and CH₂ CHFCl. The terms "halocycloalkyl", "haloalkenyl" and "haloalkynyl" are defined analogously to the term "haloalkyl".

The total number of carbon atoms in a substituent group is indicated by the "C_(i) to C_(j) " prefix where ia nd j are integers. For example, C₁ to C₃ alkylsulfonyl would designate methylsulfonyl through propylsulfonyl; C₂ alkoxyalkoxy would designate OCH₂ OCH₃ ; C₄ alkoxyalkoxy would designate the various isomers of an alkoxy group substituted with a second alkoxy group containing a total of 4 carbon atoms, examples including OCH₂ OCH₂ CH₂ CH₃ and OCH₂ CH₂ OCH₂ CH₃ ; C₂ cyanoalkyl would designate CH₂ CN and C₃ cyanoalkyl would designate CH₂ CH₂ CN and CH(CN)_(CH) ₃ ; C₂ alkylcarbonyl would designate C(O)CH₃ and C₄ alkylcarbonyl would include C(O)CH₂ CH₂ CH₃ and C(O)CH(CH₃)₂ ; and as a final example, C₃ alkoxycarbonylalkyl would designate CH₂ CO₂ CH₃ and C₄ alkoxycarbonylalkyl would include CH₂ CH₂ CO₂ CH₃, CH₂ CO₂ CH.sub. 2 CH₃ and CH(CH₃)CO₂ CH₃.

Preferred Compounds A are those of Formula I

wherein:

A is CR_(a) R_(a), S, O or NR₆ ;

B is H, C₁ to C₆ alkyl, C₁ to C₆ haloalkyl, C₂ to C₆ alkenyl, C₂ to C₆ alkynyl, C₂ to C₆ alkoxyalkyl, C₃ to C₈ alkoxycarbonylalkyl, CO₂ R₃, C(O)R₃, C(O)NR₃ R₄, C(S)NR₃ R₄, C(S)R₃, C(S)SR₃, phenyl or phenyl substituted by (R₅)p;

W is Cl, F, Br, Cn, CF₃, C₁ to C₂ alkyl, C₁ to C₂ alkoxy, OCF₂ H, OCF₃ or NO₂ ;

R₂ is R₃, halogen, CN, SCN, NO₂, OR₃ or SR₃ ;

R₃ is H, C₁ to C₄ alkyl, C₁ to C₂ haloalkyl, C₃ to C₄ alkenyl, C₃ to C₄ haloalkenyl, propargyl, phenyl, benzyl, or phenyl or benzyl substituted with one of F, Cl, Br, CF₃, OCF₃, OCF₂ H or NO₂ ;

p is 1 or 2;

m is 1 or 2;

X is O;

Y is H, C₁ to C₄ alkyl, SCH₃, SCCl₃, SO₂ CH₃, SC₆ H₅, 2--NO₂ --C₆ H₄ S, C(O)CH₃, C(O)CH₂ CH₃, C(O)CF₃ ; CO₂ CH₃, CO₂ CH₂ CH₃, or S-J;

J is J₁, J₂, J₃, J₄ or J₅ ;

R₈ and R₁₂ and independently selected from C₁ to C₆ alkyl, C₁ to C₆ haloalkyl, C₅ to C₆ cycloalkyl, C₃ to C₈ alkoxycarbonylalkyl, phenyl, benzyl and phenethyl, each phenyl, benzyl and phenethyl optionally substituted with W, or, R₈ and R₁₂ can be taken together as (CH₂)₄, (CH₂)₅ or (CH₂)₂ O(CH₂)₂ ;

R₁₀ and R₁₁ are independently selected from C₁ to C₃ alkyl or phenyl; and

t is 2.

Preferred compounds B are Compounds A wherein:

B is H, C₁ to C₄ alkyl, C₃ to C₄ alkoxycarbonylalkyl, CO₂ R₃, C(O)R₃, phenyl or phenyl substituted with (R₅)p;

R₁ is halogen, CN, SCN, NO₂, OR₃, SR₃, SO₂ R₃, CO₂ R₃, C(O)R₃ or is R₃ with one substituent in the 4-position;

R₅ is H, R₃, halogen, CN, SCN, NO₂, OR₃, SR₃, SO₂ R₃, C(O)R₃, OSO₂ R₃, CO₂ R₃, C(O)R₃, C(O)NR₃ R₄, SO₂ NR₃ R₄ or NR₃ R₄ ; or, when m or p is 2;

R₁ and R₅ can be --CH₂ C(CH₃)₂ O--, OCH₂ CH₂ O--, OCF₂ CF₂ O-- or --CH₂ CF₂ O--;

R₃ is C₁ to C₄ alkyl, C₁ to C₂ haloalkyl, C₃ to C₄ alkenyl or propargyl;

R₄ is H or CH₃ ;

R_(a) is H, CH₃, CO₂ CH₃ or CO₂ CH₂ CH₃ ;

m and p are independently 1 or 2 and one substituent is in the para-position;

Y is H, CH₃, COCH₃, CO₂ CH₃ or S-J;

J is J₁ or J₂ ;

R₈ is C₁ to C₄ alkyl or phenyl optionally substituted with Cl or CH₃ ;

R₉ is C₁ to C₂₀ alkyl, C₁ to C₂₀ alkoxy, C₁ to C₆ haloalkyl, dimethylamino, phenyl optionally substituted with Cl or CH₃, or, R₉ is C₁ to C₄ alkoxy substituted with C₂ to C₄ alkoxy or 1 to 6 halogens; and

G is S.

Preferred Compounds C are Compounds B wherein:

R₁ is Cl, F, Br, CF₃, CN, OCF₃, OCF₂ H, OCF₂ CF₂ H or SCF₂ H;

R₂ and R₅ are independently H, CL, F, Br, CN, CF₃, CH₃, OCH(CH₃)₂, OCF₂ H, OCF₃, SCH₃, SCF₂ H, NO₂ or OCH₂ CH₃ ;

B is H, CH₃, CH₂ CH₃, CH(CH₃)₂, CO₂ CH₃, CO₂ CH₂ CH₃, phenyl or phenyl substituted with (R₅)p; and

R_(a) is H or CH₃.

Preferred Compounds D are Compounds C wherein: A is O or CH₂ ;

Preferred Compounds E are Compounds D wherein: Q is Q-1;

Preferred Compounds F are Compounds D wherein: Q is Q-2;

Preferred Compounds G are Compounds D wherein: Q is Q-3;

Preferred Compounds H are Compounds D wherein: Q is Q-4;

Preferred Compounds I are Compounds D wherein: Q is Q-5;

Preferred Compounds J are Compounds D wherein: Q is Q-6;

Preferred Compounds K are Compounds D wherein: Q is Q-7;

Preferred Compounds L are Compounds D wherein: Q is Q8;

Specifically preferred compounds are:

M) methyl 3,3a,4,5-tetrahydro-2-[[[4-trifluoromethyl)pheny]-amino]carbonyl]-2H-pyrazolo[3,4-f]-quinoline-3a-carboxylate, a compound of Preferred E;

N) methyl 3,3a,4,5-tetrahydro-2-[[[4-trifluoromethyl)phenyl]-amino]carbonyl]-2H-pyrazolo[4,3-h]-quinoline-3a-carboxylate, a compound of Preferred H;

O) methyl 7-chloro-3,3a,4,5-tetrahydro-N-[[[4-trifluoromethyl)phenyl]amino]carbonyl]-2H-thieno [2,3-g]-indazole-3a-carboxylate, a compound of Preferred I;

P) methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoromethyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1-c]-[1,4]benzoxazine-3a-carboxylate, a compound of Preferred L; and

Q) 7-chloro-3A-(4-fluorophenyl)-3A,4-dihydro-N-[4-(trifluoromethyl)phenyl]-3H-pyrazolo[5,1-c][1,4]-benzoxazine-2carboxamide, a compound of Preferred L.

Hereafter, in the specification and claims, the various geometric isomers, stereoisomers and agriculturally suitable salts of each and every compound of the invention depending on context, is/are included in the term "compound(s)."

DETAILS OF THE INVENTION

For descriptive purposes, Q-1, where R_(a) is H, will be used as a representative value of Q, when Q is Q-1 through Q-7, in the discussion that follows and will be referred to by the following numbering system: ##STR12##

Compounds of Formula I can be prepared by the reaction of aryl isocyanates of Formula II and substituted indazoles of Formula III as shown in Scheme I. Typical reactions involve the combination of equimolar amounts of II and III in conventional organic solvents including ether, tetrahydrofuran (THF), methylene chloride, chloroform and benzene. The reaction can be run at temperatures ranging from about -20° C. to 100° C. with temperatures in the range of about -10° to 30° C. generally preferred. ##STR13##

Substituted indazoles of Formula III, where B is equal to H, can be prepared by the reaction of hydrazine with an α, β-unsaturated ketone of Formula IV (or their precursors) by procedures well documented in the chemical literature (Scheme 2). For a review of pyrazoline synthesis, see El-Rayyes and Al-Awadi, Synthesis, 1028 (1985). For literature describing the synthesis of 3,4- and 3,5-disubstituted pyrazolines, which can be applied to the synthesis of compounds of Formula III, where B is H, see U.S. Pat. No. 3,991,073 and U.S. Pat. No. 4,070,365. ##STR14##

Preparation of compounds of Formula I, where B is other than H, OR₇, phenyl or substituted phenyl can be achieved by metallation of the 3a position of Formula I (where B is H) followed by reaction with a suitable electrophile as depicted in Scheme 3. Procedures for the related transformation of 4-substituted pyrazolines to 4,4-disubstituted pyrazolines are reported in U.S. Pat. No. 4,663,341 and can be applied to the substituted indazoles of Formula I. Metallation can be accomplished by deprotonation with a strong base, in a suitable solvent and at temperatures ranging from -78° C. to 100° C. Useful bases for this reaction include lithium dialkylamides such as lithium diisopropylamide and lithium tetramethylpiperidide and alkyl lithium reagents such as n-butyllithium and s-butyllithium. Deprotonation of compounds of Formula I, where B is equal to hydrogen, will require two equivalents of base when Y is equal to hydrogen. The reaction can be conducted in many conventional organic solvents and in certain instances a cosolvent may be useful. Suitable solvents include diethylether, tetrahydrofuran, tetrahydropyran, benzene and the like. Suitable electrophilic reagents for reaction with the metallated Formula I compounds include alkyl and substituted alkyl halides, alkyl chloroformates, acyl halides, isocyanates, dialkyl carbamoylhalides and related electrophiles which will be known to those skilled in the art. ##STR15##

An alternative procedure for introduction of the 3a substituent, which in certain instances is preferred over that of Scheme 3 due to higher yields and/or greater ease of synthesis, proceeds via the intermediacy of Compound V, wherein the 2-nitrogen has been derivatized with a suitable protecting group. Deprotonation with a strong base such as lithium diisopropylamide, typically in stoichiometric quantities, followed by reaction with any of the previously described electrophiles provides compounds of Formula V where B is other than hydrogen, OR₇, phenyl or substituted phenyl. Removal of the nitrogen protecting group provides the required Formula III intermediate. Nitrogen-protecting groups are well documented in the chemical literature, as are procedures for their preparation and cleavage. Examples include acetyl, trifluoroacetyl, benzoyl, substituted benzoyl, alkoxycarbonyl, benzyl and substituted benzyl. For a review see Greene "Protective Groups in Organic Synthesis" (New York: John Wiley and Sons, 1981) pp. 218 to 287. ##STR16##

Formula III compounds where B is equal to hydroxy are prepared by the reaction of hydrazine with a suitably substituted epoxide of Formula VI (Scheme 5). The epoxides are available from the enones of Formula IV by procedures known in the art, the most widely employed method being epoxidation via the use of alkaline hydrogen peroxide (see, e.g., Wasson and House, Org. Syn., Coll. Vol. 4, 552 (1963)).

Compounds of Formula I where B is equal to OR₇ and R₇ is other than hydrogen, can be preferred from the Formula I compounds where B is equal to hydroxy via reaction with electrophilic reagents such as alkyl halides, acyl halides, alkyl chloroformates, chlorosulfonate, isocyanates and dialkyl carbamoylhalides. Those skilled in the art will recognize that conditions necessary for this transformation including solvent, catalyst, temperature, etc., will vary with the specific electrophile chosen and the specific Formula I compound used. ##STR17##

Compounds of Formula III where B is phenyl or substituted phenyl can be prepared by reaction of a ketone of Formula IX, where L is a suitable leaving group such as chloride, bromide, tosylate or mesylate, with hydrazine. The formula IX compounds are in turn prepared from the compounds of Formula VII in a two-step process involving first an aldol reaction of formaldehyde to produce the aldol product of Formula VIII followed by conversion of the hydroxyl group to a leaving group L. As an example, treatment of the Formula VIII compound with methanesulfonylchloride in the presence of an amine base produces the Formula IX compound where L is mesylate. ##STR18##

The α-methylene ketones of Formula IV can be prepared from the ketones of Formula X by a variety of procedures well documented in the literature. For example, treatment of X with with tetramethyldiaminomethane and acetic anhydride produces the Formula IV compound directly. Another useful procedures is to treat the Formula X compound with formaldehyde under conditions of a Mannich reaction. The dialkylamino group can be eliminated in situ upon treatment with base to form the intermediate of Formula IV. ##STR19##

Those skilled int he art will recognize the intermediates of Formula X as substituted quinolones. Isoquinolones and the isomer benzothiophenones used for preparation of compounds of Formula I, where Q is Q-2 through Q-7, are also known in the chemical literature as are procedures for their preparation. A few selected references include: where Q is Q-1 see J. Chem. Soc., Perkin I, 975 (1976), where Q is Q-2 see J. Amer. Chem. Soc., 107, 4998 (1985), where Q is Q-3 see J. Org. Chem. 43, 966 (1978), where Q is Q-4 see J. Het. Chem. 15, 249 (1978), when Q is Q-5 or Q-7 see Tetrahedron Letters, 2885 (1975) or J. Heterocyclic Chem., 17, 87 (1980), and where Q is Q-6 see Bull. Soc. Chim. Fr., 335 (1973).

An alternative method for preparing compounds of Formula I, where Q is Q-1 through Q-7, involves intramolecular cyclization of hydrazone XI or produce the N-phosphorylated dihydropyrazole XII. The phosphorus group can then be removed under acidic conditions and neutralized with base to yield the substituted indazoles of Formula III. ##STR20## wherein: R_(x) and R_(y) are independently selected from C₁ to C₄ alkyl and C₁ to C₄ alkoxy.

The intramolecular cyclization can be conducted by gradual addition of a moderately reactive halogenating agent such as N-chlorosuccinimide to a mixture of a base, such as triethylamine, and the compound of Formula XI in a dry inert solvent such as ether, dichloromethane or toluene. Alternatively, when Q is Q-5, Q-6 or Q-7, the base can be added gradually to a mixture of the halogenating agent and compound XI. It is preferable that the concentration of reactant be kept relatively low (0.01 to 0.5 M) and that the compound being added to the reaction mixture is added gradually to avoid competing side reactions which occur at higher concentrations. For optimum yields, it is also important to maintain anhydrous conditions.

Hydrolysis of the phosphorus group is best accomplished by treatment of XII with 1 t 5 equivalents of a strong acid such as hydrochloric, sulfuric or p-toluenesulfonic in a suitable solvent such as methanol, ethanol or tetrahydrofuran, optionally containing about 0.1 to 10 equivalents of water. The reaction can be conducted at temperatures generally ranging from about 20° to 100° C. with the reflux temperature of the solvent being generally preferred. Once the reaction is complete, the acid salt can be precipitated by cooling to 0° C., or if it does not precipitate, the solvent can be removed and ether added to facilitate crystallization. The acid salt of III can then be neutralized with an inorganic base such as sodium carbonate or sodium bicarbonate to give the free base III. In some instances, it is preferable to convert the acid salt of III directly to compounds of Formula I by addition of an aqueous solution of an inorganic base to a suspension of the salt III in an organic solvent such as tetrahydrofuran, followed by addition of the isocyanate II.

Compounds of Formula XI are prepared by condensation of an aldehyde of Formula XIII with a phosphorus hydrazid of Formula XIV. ##STR21##

This reaction is typically run in an inert organic solvent. Alcohol solvents such as methanol and ethanol and ether solvent such as tetrahydrofuran and diethyl ether are generally preferred. The reaction can also be conducted with a catalytic amount of acid such as p-toluenesulfonic acid although typically acid catalysis is not necessary. The products of Formula XI generally precipitate from the reaction mixture as they are formed.

Starting materials of Formula XIII and XIV can be prepared by analogy with procedures known in the art.

Compounds of Formula I, where Q is Q-8, can be obtained by the reaction of activated carbonyl or thiocarbonyl compounds of Formula II with substituted anilines in the presence or absence of an acid acceptor or suitable condensing agent. Methods for performing this transformation as well known in the art; see, Zabicky, "The Chemistry of the Amides", Interscience, 1970.

One particularly useful method involves the chlorination of an acid derivative (XV, X₁ =OH) with thionyl chloride or another chlorinating agent followed by treatment with an aniline (XVI) in the presence of an acid acceptor such as an amine base, preferably triethylamine. Suitable solvents for the chlorination reaction are inert to hydrogen chloride and include benzene, toluene, and dichloromethane. Preferred temperatures for this process are from 20° to 100° C. with temperatures between 20° and 80° C. being particularly preferred. The latter reaction can be carried out in many different inert solvents such as dialkylethers, chlorinated hydrocarbons, and aromatic hydrocarbons. While temperatures at or below 25° C. are preferred, higher temperatures can also be employed. These reactions are normally run at atmospheric pressure, but can also be carried out at elevated pressures. ##STR22##

Esters of Formula XV (X₁ =C₁ to C₆ alkoxy) can be converted directly to compounds of Formula I (Q=Q-8) in several ways. In the presence of Lewis acids such as AlMe₃, anilines react readily with esters of Formula XV. The reaction is best carried out at room temperature to 120° C. Suitable solvents include dichloromethane, 1,2-dichloroethane, and toluene. The method described by Weinreb et al., Organic Synthesis, 59, 49, (1982), proceeds best with esters of lower alcohols such as methanol and ethanol.

Acids of Formula XV (X₁ =OH) can be converted directly to compounds of Formula I by use of coupling agents known in the peptide art in conjunction with anilines. Coupling agents include dicyclohexylcarbodiimide (DCC), N-hydroxysuccinimide, 2-chloro-N-methylpyridinium iodide, carbonyl diimidazole, or other agents capable of activating an acid function or acting as a dehydrating agent. These and other methods are described in Gross et al., "The Peptides," 3 Vols., Academic Press, New York, 1979 to 1981.

Compounds of Formula I (Q=Q-8) and intermediates of Formula XV can also be obtained by the intramolecular dipolar cycloaddition reaction of nitrile-imines, generated from substituted phenylhydrazones of Formula XVII (Scheme 11). The presence of an acid acceptor (generally an amine base, for example, triethylamine) is necessary for the formation of the nitrile-imine. Suitable solvents include but are not restricted to benzene, toluene, 1,2-dichloroethane, chloroform, and tetrahydrofuran. The reaction can be carried out at temperatures ranging from 20° to 120° C. with the relative reactivity of the alkene moiety governing the required temperature for a given example. ##STR23##

The required hydrazones of Formula XVII can be synthesized by the Japp-Klingemann reaction (Scheme 12). The coupling of diazonium salts with active methylene compounds is known. The more specific coupling of chloroacetoacetic acid derivatives of Formula XVIII with diazotized anilines of Formula XVIV containing alkenyl substituents is described by Padwa et al. in J. Org. Chem., 43, 1664 (1978) and J. Org. Chem., 46, 1402 (1981). A similar process for this type of aniline is described by Garanti et al. in J. Org. Chem., 42, 1389 (1977), and J. Chem. Soc. Perkin I, 2245 (1981). ##STR24##

The anilines of Formula XVIV can be obtained by the reduction of aromatic nitro compounds of Formula XX (Scheme 13). There are many methods known for this transformation. See, March, "Advanced Organic Chemistry", 1985, Wiley, page 1103-1104. A particularly suitable method involves the treatment of the nitro compound with tin (II) chloride in alcoholic solvents. Refer to Bellamy et al. Tetrahedron Letters, 1984, 839. ##STR25##

Nitro compounds of Formula XX containing a heteroatom in the alkenyl chain can be obtained by alkylation reactions (Scheme 14). Treatment of a substituted phenol, thiophenol, or aniline or Formula XXI with an acid acceptor and an alkyl or homoallyl halide or sulfonate of Formula XXII gives compounds of Formula XX as products. Preferred acid acceptors for the process are inorganic bases such as potassium carbonate. Preferred solvents include dimethylformamide, dimethylsulfoxide, methylethyl ketone, and ethanol. The reaction is generally carried out at room temperature, but higher temperatures may be necessary in some cases. Alternative methods for these nitro compounds of Formula XX have been described by Oae et al. in Bull. Chem. Jap., 54, 2374 (1981). ##STR26##

Anilines of Formula XVIV containing sulfur can be obtained by alkylation on the sulfur of Formula XXIII (Scheme 15). The conditions which favor this process are alcoholic solvents and sodium hydroxide or sodium alkoxides as bases. The reaction is generally carried out using a allylic halides of Formula XXII at 20° to 80° C. in lower alcoholic solvents, preferably ethanol. ##STR27##

Anilines of Formula XVIV which do not contain a heteroatom in the alkenyl portion can be synthesized by the Claisen rearrangement (Scheme 16). The thermal and acid catalyzed rearrangement of N-allylanilines of Formula XXIV has been described by Hansen et al. in Helv. Chim. Acta., 60, 978 (1977). ##STR28##

The hydrazonyl halides of Formula XVII (A=S, q-1 or 2) in which a sulfoxide or sulfone are present may be obtained by the oxidation of the corresponding sulfide of Formula XVII (A=S, q=O) (Scheme 17). Oxidation of hydrazones of Formula XVII (A=S), q=O) by hydrogen peroxide in acetic acid is known. See Zecchi et al., J. Chem. Res. 1887 (1986). By modifications of the amount of oxidant, reaction time and temperature the product obtained can be specifically the sulfoxide of Formula XVII (A=S, q-1) or the sulfone of Formula XVII (A=S, q=2). ##STR29##

Cycloaddition of the hydrazones of Formula XVII (A=S, q=O) proceeds only in low yield. Synthesis of sulfur containing compounds XV (A=S, q=O) can be accomplished by reducing the sulfoxides of Formula XV (A=S, q=1) (Scheme 18). Many reagents are known in the art to reduce sulfoxides. See March, "Advanced Organic Chemistry", 1985, Wiley, page 1108. One particularly useful method uses titanium (III) chloride at room temperature and was described by Ho in Synthetic Comm., 3, 37 (1973). ##STR30##

Compounds of Formula I, where Y is H and Q is Q-1 through Q-8, can be converted to other compounds of Formula I by alkylation, acylation, and sulphenylation reactions to form derivatives where Y is other than H. Reaction of compounds of Formula I in the presence of an acid acceptor with electrophilic agents results in substitution on nitrogen. Strong bases such as sodium hydride, potassium t-butoxide, potassium hydride, and other bases known in the art to deprotonate amides are preferred in the process. Suitable electrophiles include, but are not restricted to alkyl halides, acyl halides, acid anhydrides, carbonates, chloroformate, disulphides, and sulphenyl halides. This reaction is normally run in the the temperature range of 0°-25° C., but can be run at temperature up to 120° C. if unreactive electrophiles are used. Solvents not deprotonated under the reactions conditions such as tetrahydrofuran, dimethylformamide, dimethoxyethane, and diethyl ether are preferred.

Compounds of Formula I (X=O) can be converted to compounds of Formula I (X=S) by means of thiating agents. Conversion of amides to thioamides is well known in the art. Phosphorous pentasulfide either alone or in combination with organic or inorganic bases is a preferred reagent to effect this conversion. When phosphorous pentasulfide is used alone, organic bases such as pyridine are the preferred solvents. When it is used in conjunction with inorganic bases such as sodium bicarbonate, the preferred solvents are ethers such as diglyme. Temperatures between 20° to 160° C. can be employed successfully with temperatures between 90° to 120° C. preferred. These and other means to convert amides to thioamides are described by Lapucha, Synthesis, 256 (1987).

The following Examples further illustrate the invention.

EXAMPLE 1 3,3A,4,5-tetrahydro-N-[4-(trifluoromethyl)phenyl]-2H-thieno[2,3-glindazole-2-carboxamide Step A: 6,7-Dihydro-5-methylenebenzo[b]thiophen-4(5H)-one

To 20.0 mL of tetramethyldiaminomethane was added 10.0 g of 6,7-dihydrobenzo[b]thiophen-4(5H)-one all at once. To this mixture was added 20.0 mL of acetic anhydride, dropwise. The reaction mixture exothermed to 45° C. and was heated to 122° C. for 15 minutes and then cooled to 90° C. where it was kept for 60 minutes. The dark solution was poured into cold water and extracted with ether. The ether was extracted with a saturated solution of NaHCO₃ and then washed with brine. The ether layer was dried over anhydrous magnesium sulfate, filtered and concentrated in vacuo to afford a yellow oil. The yellow oil was flash-chromatographed using 10% ethyl acetate and 90% hexanes as eluent to afford 6.18 g of a white solid, m.p. 47°-49° C. 200 MHz¹ H NMR(CDCl₃) δ2.97 (t, 2H), 3.07 (t, 2H), 5.46 (s, 1H), 6.17 (s,1H), 7.11 (d, 1H), 7.48 (d, 1H); I. R. (Nugol) 1660 cm⁻¹.

Step B: 3,3a,4,5-tetrahydro-2H-thieno[2,3-g]indazole

To 20 mL of anhydrous ethanol was added 1.2 g of the product from Step A and 0.40 g of hydrazine hydrate. The reaction mixture was heated at reflux for 2 h, cooled, poured into cold water and extracted with ether. The ether extracts were washed with water and brine, dried over anhydrous magnesium sulfate, filtered and utilized without concentration or purification in Step C.

Step C

Preparation of title compound was as follows. To a 150 mL solution of the product from Step B in ether was added 1.50 g of α,α,α-terifluoro-p-tolylisocyanate. The reaction mixture was stirred at room temperature for 1 hr. where a precipitate was formed. The reaction mixture was filtered and the precipitate was washed with ether to afford 0.20 g of a white solid, m.p. 219°-221° C. 200 MHz¹ H NMR(CDCl₃) δ1.98 (bm, 1H), 2.48 (bm, 1H), 3.10 (m, 2H), 3.42 (m, 2H), 4.43 (m, 1H), 7.25 (d, 1H), 7.36 (d, 1H), 7.56 (d, 2H), 7.67 (d,2H), 8.18 (bs, 1H); I.R. (Nujol) 3370,1668 cm⁻¹.

EXAMPLE 2 7-Chloro-3a,4,-dihydro-3a-phenyl-N-[4-(trifluoromethyl)phenyl)-3H-pyrazolo[5,1-c][1,4] benzoxazine-2-carboxamide Step A: 4-chloro-1-nitro-2-(phenyl-2-propenyloxy)benzene

A solution of 5-chloro-2-nitrophenol (7 g) in dimethylformamide (40 ml) was stirred at room temperature with 1-bromo-2-phenyl-2-propene (8 ml) and potassium carbonate (5.5 g) for 18 h. The reaction mixture was diluted with water (200 ml) was extracted with ether (100 ml). The ether was washed with water (3×100 ml). The solvent was removed under reduced pressure and the residue was crystallized from hexanes. The yellow solid (8.6 g) was the desired product. m.p. 74.5°-75.5° C.

NMR (200 MHz) CDCl₃ ; δ7.8 (d, 1H,ArH), 7.4-7.0 (m, 7H, ArH), 5.6 (S,S, 2H, CH₂), 5.0 (S, 2H, CH₂ O).

Step B: 4-chloro-2-[(2-phenyl-2-propenyl)oxyl]benzenamine

The compound of Step A (7.2 g) was added to a suspension of tin (II) chloride (28 g) in ethanol (45 ml). The mixture was refluxed for 1.5 h. The reaction was diluted with ethyl acetate and neutralized by careful addition of saturated sodium bicarbonate solution. The organic solution was washed with brine and the solvent was dried over magnesium sulfate. Evaporation of the solution left a thick oil of the title compound (5.8 g).

NMR (200 MHz) CDCl₃ δ7.4-6.6 (m, 8H, ArH), 5.6-5.4 (S,S, 2H, CH₂), 4.9 (S, 2H, CH₂ O), 3.2 (Br, NH₂).

Step C: methyl chloro [[4-chloro-2[(2-phenyl-2-propenyl)oxy]phenyl]hydrazono]acetate

Using the procedure of Example 4 (Step B), the compound of Step B (5.6 g) was converted to the title compound (2.8 g). The chromatography was carried out with hexanes/ethyl acetate (8:1); m.p. 88°-90° C.

NMR (200 MHz) CDCl₃ δ8.6 (br. s, NH₂), 7.3-6.9 (m, 8H, ArH), 5.7-5.6 (m, 2H, CH₂), 4.9 (s, 2H, CH₂ O).

Step D: methyl 7-chloro-3a-4-dihydro-3a-phenyl-3H-pyrazolo[5, 1-c[]1,4]benzoxazine-2-carboxylate

The compound of Step C (2.5 g) was dissolved in benzene (100 ml), treated with triethylamine (5 ml), and heated at reflux for 24 h. The cooled mixture was diluted with ethyl acetate (100 ml) and 1N HCL (100 ml). The organic layer was dried and evaporated. The residue was chromatographed on silica gel with hexane/ethyl acetate (5:1). The title compound (1 g) was a solid. m.p. 145°-146° C.

NMR (200 MHz) CDCl₃ δ7.6-6.8 (m, 8H, ArH), 4.65 (d, 1H, CH), 3.9 (d, 1H, CH), 3.8 (S, 3H, CH₃), 3.4 (m, 2H, CH₂).

Step E

Preparation of title compound was as follows. The compound of Step D (1.0 g) was suspended in methanol (10 ml) and treated with 50% aqueous sodium hydroxide (1 ml) and heated to reflux for 10 min. The mixture was acidified and extracted with ethyl acetate. The dried organic extract was evaporated. The residue was dissolved in benzene (15 ml) and treated with thionyl chloride (1.5 ml). The mixture was heated to reflux for 2H and then evaporated. The residue was dissolved in tetrahydrofuran (20 ml) and one half was added to a solution of p-trifluoromethoxyaniline (0.4 g) and triethylamine (1.0 ml) in tetrahydrofuran (10 ml). After stirring for 1h the mixture was partitioned between ethyl acetate (50 ml) and 1N HCl (50 ml). The dried organic layer was evaporated. Chromatography of the residue on silica gel in hexanes/ethyl acetate (7:1) gave the title compound (0.39 g). m.p. 140°-146° C.

NMR (200 MHz) CDCl₃ δ8.6 (br, NH), 7.8-6.9 (m, 12H, ArH), 4.7 (d, 1H, CH), 3.8 (d, 1H, CH), 3.4 (dd, 2H, CH₂).

EXAMPLE 3 Methyl 7-fluoro-3a,4-dihydro-2-[[[4-(trifluoromethyl)phenyl]amino]carbonyl]-3H-pyrazolo[5,1-c]-[1,4]benzoxazine-3a-carboxylate Step A: methyl 2-[(5-fluoro-2-nitrophenoxy) methyl]-2-propenoate

The compounds 5-fluoro-2-nitrophenol (8.0 g), methyl 2-bromomethylacrylate (9.5 g) and potassium carbonate (7 g) under the conditions of Example 2, (Step A) gave the title compound (11.6 g). m.p. 89°-92° C.

NMR (200 MHz) CDCl₃ δ8.0 (m, 1H, ArH), 6.9 (m,2H, ArH), 6.4-6.2 (S,S, 2H, CH₂), 4.8 (S, 2H, CH₂ O), 3.8 (S, 3H, CH₃ O).

Step B: methyl 2-[(2-amino-5-fluorophenoxy)methyl]-2-propenoate

The compound of Step A (11.0 g) was converted to the title compound (8 g) by the method of the Example 2 (Step B).

NMR (200 MHz) CDCl₃ δ6.8 (m, 3H, ArH), 6.5 & 6.0 (S, S, 2H, CH₂), 4.8 (S, 2H, CH₂ O), 4.2 (Br, NH₂), 3.8 (S, 3H, CH₃ O).

Step C: methyl 2-[[2-[2-(1-chloro-2-methoxy-2-oxo-ethylidene)hydrazino]-5-fluorophenoxy]methyl]-2-propenoate

Using the procedure of Example 4 (Step C) the title compound (2.1 g) was prepared from the compound of Step B (7.5 g).

NMR (200 MHz) CDCl₃ δ8.7 (br. s, NH), 7.6 (m, 1H, ArH), 6.9 (m, 2H, ArH), 6.5 (S, 1H, CH₂), 6.0 (S, 1H, CH₂), 4.8 (S, 2H, CH₂), 3.8 (S, 6H, 2OCH₃).

Step D

Preparation of title compound (0.13 g) was as follows. The procedure of Example 2 (Steps D and E) were used with the compound of Step C (1.8 g) and the p-trifluoromethoxyaniline was replaced with p-trifluoromethyl-aniline. m.p. 177.5°-181° C.

NMR (200 MHz) CDCl₃ δ8.6 (br, NH), 7.7-6.8 (m, 7H, ArH), 4.7 (d, 1H, CH₂ O), 3.8 (S, 3H, CH₃ O), 3.8-3.4 (m, 3H, CH₂, CH₂ O).

EXAMPLE 4 Methyl 3a,4-dihydro-3a-phenyl-3H-pyrazolo[5,1-c[]1,4]benzothiazine-2-carboxylate-5-oxide Step A: 2-[(2-phenyl-2-propenyl)thio]benzenamine

The compound, 2-aminothiophenol, (12.5 g) was added to a solution of sodium hydroxide (4.5 g) in ethanol (100 ml) keeping the temperature less than 30° C. Then 1-bromo-2phenyl-2-propene (21 g) was added and the mixture was stirred at 60° C. for 3 h. The precipitated solid was filtered and washed with ethanol. The solvent was removed and the residue was chromatographed on silica gel with hexanes/ethyl acetate (7:1) to yield the title compound (14.5 g). As an oil.

NMR (200 MHz) CDCl₃ δ7.3-7.0 (m, 9H, ArH), 5.3-5.0 (m, 2H, CH₂), 4.0 (Br, NH₂), 3.8 (S, 2H, CH₂ S).

Step B: methyl chloro[[2-[(2-phenyl-2-propenyl)thio]-phenyl]hydrazono]acetate

The compound of Step A (14.5 g) was treated with 6N HCl (22 ml) and water (100 ml). This mixture was cooled to below 0° C. and treated dropwise with an aqueous solution of sodium nitrite (4.2 g). The resulting mixture was decanted into an insulated dropping funnel. The mixture was added to a cooled (-5° to -10° C.) mixture of sodium acetate (15 g) and methyl 2-chloroacetoacetate (5 ml) in ethanol (100 ml) so that the internal temperature did not exceed 5° C. The mixture was allowed to come to room temperature over 2 h and then extracted with ether. The dried organic layer was evaporated and chromatographed on silica el with ether/hexanes (1:2). The title compound (11.5 g) was isolated as a yellow oil. NMR (200 MHz) CDCl₃ δ9.4 (br, NH) 7.5-7.0 (m, 9H, ArH), 5.2 (S, 1H, CH₂), 4.8 (S, 1H, CH₂), 3.9 (S, 3H, CH₃), 3.8 (S, 2H, CH₂ S).

Step C: methyl chloro[[2-[(2-phenyl-2-propenyl)sulfinyl]phenyl]-hydrazono]acetate

The compound of Step B (5 g) was stirred with occasional warming in acetic acid (45 ml) and treated with 30% aqueous hydrogen peroxide (2.0 ml). After stirring for 5 h, water (200 ml) was added and the P.h. was adjusted to 6 with sodium bicarbonate. Saturated sodium bisulfite solution (3 ml) was added and the mixture was extracted with dichloromethane (200 ml). The organic layer was dried and evaporated to give the title compound (4.9 g).

NMR (200 MHz) CDCl₃ δ7.6-7.0 (m, 9H, ArH), 5.6-4.2 (m, 4H, CH₂), 4.0 (S, 3H, CH₃ O).

Step D

Preparation of title compound (1.0 g) was as follows. The method of Example 2 (Step D) was applied to the compound of Example 12 (4.5 g). Purification was accomplished by chromatography on silica gel with hexanes/ethyl acetate (1:1).

NMR (200 MHz) CDCl₃ δ7.3-7.0 (m, 9H, ArH), 4.2 (dd, 1H, CH₂), 3.9 (S, CH₃ O, 3H), 3.6 (m, 3H, CH₂).

EXAMPLE 5 3a,4-Dihydro-3a-phenyl-N-[4-(trifluoromethyl)phenyl]-3H-pyrazolo[5,1-c]benzothiazine-2-carboxamide

The compound of Example 4 (Step D) (1 g) was treated with 20% aqueous titanium (III) chloride (2 ml) in dichloromethane (20 ml) and methanol (20 ml). The mixture was stirred for 20 min. at room temperature and partitioned between ethyl acetate (150 ml) and water (200 ml). The dried organic phase was concentrated and the residue was subjected to the conditions of Example 10 with p-trifluoromethylaniline in place of p-trifluoromethoxyaniline. The title compound (0.6 g) was isolated as a solid. m.p. 238°-240° C.

NMR (200 MHz) CDCl₃ δ8.6 (br, NH), 7.8-6.9 (m, 13H, ArH), 3.6 (S, 2H, CH₂), 3.4 (S, 2H, CH₂).

By the general procedures described herein, or obvious modifications thereof, the compounds of Tables 1through 16 can be prepared.

    ______________________________________                                         SUMMARY OF TABLES                                                              ______________________________________                                         Table     Q              Y     G                                               ______________________________________                                         1         Q-1            H     --                                              2         Q-2            H     --                                              3         Q-3            H     --                                              4         Q-4            H     --                                              5         Q-5            H     S                                               6         Q-6            H     S                                               7         Q-7            H     S                                               8         Q-5            H     O                                               9         Q-6            H     O                                               10        Q-7            H     O                                               Table 11   R.sub.a is H, X is O, G is S                                        Table 12   R.sub.a is H, X is O, G is S, Y is S--J                             Table 13   Q is Q-8, R.sub.a is H, Y is H, A is CH.sub.2                       Table 14   Q is Q-8, R.sub.a is H, Y is H                                      Table 15   Q is Q-8, R.sub.a is H                                              Table 16   Q is Q-8, Y is H                                                    ______________________________________                                    

In the Tables that follow, the values of Q will be referred to by the following numbering system: ##STR31##

                  TABLE 1                                                          ______________________________________                                                                                 R.sub.a.sup.1,                         R.sub.1   R.sub.2  A      B         X   R.sub.a.sup.2                          ______________________________________                                         4-CF.sub.3                                                                               H        CH.sub.2                                                                              H         O   H, H                                   4-Cl      H        CH.sub.2                                                                              H         O   H, H                                   4-Br      H        CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              H         O   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              H         O   H, H                                   4-Br      5-Cl     CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               5-F      CH.sub.2                                                                              H         O   H, H                                   4-Cl      5-F      CH.sub.2                                                                              H         O   H, H                                   4-Br      5-F      CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               5-CN     CH.sub.2                                                                              H         O   H, H                                   4-Cl      5-CN     CH.sub.2                                                                              H         O   H, H                                   4-Br      5-CN     CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               5-Br     CH.sub.2                                                                              H         O   H, H                                   4-Cl      5-Br     CH.sub.2                                                                              H         O   H, H                                   4-Br      5-Br     CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               5-Me     CH.sub.2                                                                              H         O   H, H                                   4-Cl      5-Me     CH.sub.2                                                                              H         O   H, H                                   4-Br      5-Me     CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               7-F      CH.sub.2                                                                              H         O   H, H                                   4-Cl      7-F      CH.sub.2                                                                              H         O   H, H                                   4-Br      7-F      CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               5-NMe.sub.2                                                                             CH.sub.2                                                                              H         O   H, H                                   4-Cl      5-NMe.sub.2                                                                             CH.sub.2                                                                              H         O   H, H                                   4-Br      5-NMe.sub.2                                                                             CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               5-CF.sub.3                                                                              CH.sub.2                                                                              H         O   H, H                                   4-Cl      5-CF.sub.3                                                                              CH.sub.2                                                                              H         O   H, H                                   4-Br      5-CF.sub.3                                                                              CH.sub.2                                                                              H         O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              Me        O   H, H                                   4-Cl      H        CH.sub.2                                                                              Me        O   H, H                                   4-Br      H        CH.sub.2                                                                              Me        O   H, H                                   4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              Me        O   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              Me        O   H, H                                   4-Br      5-Cl     CH.sub.2                                                                              Me        O   H, H                                   4-CF.sub.3                                                                               5-CF.sub.3                                                                              CH.sub.2                                                                              Me        O   H, H                                   4-Cl      5-CF.sub.3                                                                              CH.sub.2                                                                              Me        O   H, H                                   4-Br      5-CF.sub.3                                                                              CH.sub.2                                                                              Me        O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              Et        O   H, H                                   4-Cl      H        CH.sub.2                                                                              Et        O   H, H                                   4-Br      H        CH.sub.2                                                                              Et        O   H, H                                   4-CF.sub.3                                                                               5-F      CH.sub.2                                                                              Et        O   H, H                                   4-Cl      5-F      CH.sub.2                                                                              Et        O   H, H                                   4-Br      5-F      CH.sub.2                                                                              Et        O   H, H                                   4-CF.sub.3                                                                               5-CN     CH.sub.2                                                                              Et        O   H, H                                   4-Cl      5-CN     CH.sub.2                                                                              Et        O   H, H                                   4-Br      5-CN     CH.sub.2                                                                              Et        O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              allyl     O   H, H                                   4-Cl      H        CH.sub.2                                                                              allyl     O   H, H                                   4-Br      H        CH.sub.2                                                                              allyl     O   H, H                                   4-CF.sub.3                                                                               5-Br     CH.sub.2                                                                              allyl     O   H, H                                   4-Cl      5-Br     CH.sub.2                                                                              allyl     O   H, H                                   4-Br      5-Br     CH.sub.2                                                                              allyl     O   H, H                                   4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              allyl     O   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              allyl     O   H, H                                   4-Br      5-Cl     CH.sub.2                                                                              allyl     O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Cl      H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Br      H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               5-F      CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Cl      5-F      CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Br      5-F      CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Br      5-Cl     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               5-Br     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Cl      5-Br     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Br      5-Br     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               5-CN     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Cl      5-CN     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Br      5-CN     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               5-CF.sub.3                                                                              CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Cl      5-CF.sub.3                                                                              CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Br      5-CF.sub.3                                                                              CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               5-Me     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Cl      5-Me     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Br      5-Me     CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 Et                                                                              O   H, H                                   4-Cl      H        CH.sub.2                                                                              CO.sub.2 Et                                                                              O   H, H                                   4-Br      H        CH.sub.2                                                                              CO.sub.2 Et                                                                              O   H, H                                   4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              CO.sub.2 Et                                                                              O   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              CO.sub.2 Et                                                                              O   H, H                                   4-Br      5-Cl     CH.sub.2                                                                              CO.sub.2 Et                                                                              O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 -i-Pr                                                                           O   H, H                                   4-Cl      H        CH.sub.2                                                                              CO.sub.2 i-Pr                                                                            O   H, H                                   4-Br      H        CH.sub. 2                                                                             CO.sub.2 i-Pr                                                                            O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CF.sub.3                                                               O   H, H                                   4-Cl      H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CF.sub.3                                                               O   H, H                                   4-Br      H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CF.sub.3                                                               O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 allyl                                                                           O   H, H                                   4-Cl      H        CH.sub.2                                                                              CO.sub.2 allyl                                                                           O   H, H                                   4-Br      H        CH.sub.2                                                                              CO.sub.2 allyl                                                                           O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O   H, H                                   4-Cl      H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O   H, H                                   4-Br      H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              Ph        O   H, H                                   4-Cl      H        CH.sub.2                                                                              Ph        O   H, H                                   4-Br      H        CH.sub.2                                                                              Ph        O   H, H                                   4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              Ph        O   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              Ph        O   H, H                                   4-Br      5-Cl     CH.sub.2                                                                              Ph        O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              4-ClPh    O   H, H                                   4-Cl      H        CH.sub.2                                                                              4-ClPh    O   H, H                                   4-Br      H        CH.sub.2                                                                              4-ClPh    O   H, H                                   4-CF.sub. 3                                                                              5-CF.sub.3                                                                              CH.sub.2                                                                              4-ClPh    O   H, H                                   4-Cl      5-CF.sub.3                                                                              CH.sub.2                                                                              4-ClPh    O   H, H                                   4-Br      5-CF.sub.3                                                                              CH.sub.2                                                                              4-ClPh    O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              4-FPh     O   H, H                                   4-Cl      H        CH.sub.2                                                                              4-FPh     O   H, H                                   4-Br      H        CH.sub.2                                                                              4-FPh     O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              H         O   Me, H                                  4-Cl      H        CH.sub.2                                                                              H         O   Me, H                                  4-Br      H        CH.sub.2                                                                              H         O   Me, H                                  4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              H         O   Me,                                                                            Me                                     4-Cl      5-Cl     CH.sub.2                                                                              H         O   Me,                                                                            Me                                     4-Br      5-Cl     CH.sub.2                                                                              H         O   Me,                                                                            Me                                     4-CF.sub.3                                                                               H        CH.sub.2                                                                              H         S   H, H                                   4-Cl      H        CH.sub.2                                                                              H         S   H, H                                   4-Br      H        CH.sub.2                                                                              H         S   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              Me        S   H, H                                   4-Cl      H        CH.sub.2                                                                              Me        S   H, H                                   4-Br      H        CH.sub.2                                                                              Me        S   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 Me                                                                              S   H, H                                   4-Cl      H        CH.sub.2                                                                              CO.sub.2 Me                                                                              S   H, H                                   4-Br      H        CH.sub.2                                                                              CO.sub.2 Me                                                                              S   H, H                                   4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              H         S   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              H         S   H, H                                   4-Br      5-Cl     CH.sub.2                                                                              H         S   H, H                                   4-CF.sub.3                                                                               5-Cl     CH.sub.2                                                                              Me        S   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              Me        S   H, H                                   4-Br      SCl      CH.sub.2                                                                              Me        S   H, H                                   4-CF.sub.3                                                                               SCl      CH.sub.2                                                                              CO.sub.2 Me                                                                              S   H, H                                   4-Cl      5-Cl     CH.sub.2                                                                              CO.sub.2 Me                                                                              S   H, H                                   Br        5-Cl     CH.sub.2                                                                              CO.sub.2 Me                                                                              S   H, H                                   4-CF.sub.3                                                                               5-Me     CH.sub.2                                                                              H         S   H, H                                   4-Cl      5-Me     CH.sub.2                                                                              H         S   H, H                                   4-Br      5-Me     CH.sub.2                                                                              H         S   H, H                                   4-CF.sub.3                                                                               H        O      H         O   H, H                                   4-Cl      H        O      H         O   H, H                                   4-Br      H        O      H         O   H, H                                   4-CF.sub.3                                                                               5-Cl     O      H         O   H, H                                   4-Cl      5-Cl     O      H         O   H, H                                   4-Br      5-Cl     O      H         O   H, H                                   4-CF.sub.3                                                                               5-Br     O      H         O   H, H                                   4-Cl      5-Br     O      H         O   H, H                                   4-Br      5-Br     O      H         O   H, H                                   4-CF.sub.3                                                                               5-CF.sub.3                                                                              O      H         O   H, H                                   4-Cl      5-CF.sub.3                                                                              O      H         O   H, H                                   4-Br      5-CF.sub.3                                                                              O      H         O   H, H                                   4-CF.sub.3                                                                               H        O      Me        O   H, H                                   4-Cl      H        O      Me        O   H, H                                   4-Br      H        O      Me        O   H, H                                   4-CF.sub.3                                                                               5-Cl     O      Me        O   H, H                                   4-Cl      5-Cl     O      Me        O   H, H                                   4-Br      5-Cl     O      Me        O   H, H                                   4-CF.sub.3                                                                               5-Br     O      Me        O   H, H                                   4-Cl      5-Br     O      Me        O   H, H                                   4-Br      5-Br     O      Me        O   H, H                                   4-CF.sub.3                                                                               5-CF.sub.3                                                                              O      Me        O   H, H                                   4-Cl      5-CF.sub.3                                                                              O      Me        O   H, H                                   4-Br      5-CF.sub.3                                                                              O      Me        O   H, H                                   4-CF.sub.3                                                                               5-F      O      Me        O   H, H                                   4-Cl      5-F      O      Me        O   H, H                                   4-Br      5-F      O      Me        O   H, H                                   4-CF.sub.3                                                                               H        O      CO.sub.2 Me                                                                              O   H, H                                   4-Cl      H        O      CO.sub.2 Me                                                                              O   H, H                                   4-Cl      H        O      CO.sub.2 Me                                                                              O   H, H                                   4-Br      H        O      CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               5-Cl     O      CO.sub.2 Me                                                                              O   H, H                                   4-Cl      5-Cl     O      CO.sub.2 Me                                                                              O   H, H                                   4-Br      5-Cl     O      CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               H        O      Ph        O   H, H                                   4-Cl      H        O      Ph        O   H, H                                   4-Br      H        O      Ph        O   H, H                                   4-CF.sub.3                                                                               5-Br     O      Ph        O   H, H                                   4-Cl      5-Br     O      Ph        O   H, H                                   4-Br      5-Br     O      Ph        O   H, H                                   4-CF.sub.3                                                                               H        O      H         O   Me,                                                                            Me                                     4-Cl      H        O      H         O   Me,                                                                            Me                                     4-Br      H        O      H         O   Me,                                                                            Me                                     4-CF.sub.3                                                                               H        O      H         O   H, Me                                  4-Cl      H        O      H         O   H, Me                                  4-Br      H        O      H         O   H, Me                                  4-CF.sub.3                                                                               H        O      H         O   H, Ph                                  4-Cl      H        O      H         O   H, Ph                                  4-Br      H        O      H         O   H, Ph                                  4-CF.sub.3                                                                               H        O      H         O   H,                                                                             CO.sub.2 Me                            4-Cl      H        O      H         O   H,                                                                             CO.sub.2 Me                            4-Br      H        O      H         O   H,                                                                             CO.sub.2 Me                            4-CF.sub.3                                                                               H        O      H         S   H, H                                   4-Cl      H        O      H         S   H, H                                   4-Br      H        O      H         S   H, H                                   4-CF.sub.3                                                                               H        S      H         O   H, H                                   4-Cl      H        S      H         O   H, H                                   4-Br      H        S      H         O   H, H                                   4-CF.sub.3                                                                               5-Cl     S      H         O   H, H                                   4-Cl      5-Cl     S      H         O   H, H                                   4-Br      5-Cl     S      H         O   H, H                                   4-CF.sub.3                                                                               5-Br     S      H         O   H, H                                   4-Cl      5-Br     S      H         O   H, H                                   4-Br      5-Br     S      H         O   H, H                                   4-CF.sub.3                                                                               5-CF.sub.3                                                                              S      H         O   H, H                                   4-Cl      5-CF.sub.3                                                                              S      H         O   H, H                                   4-Br      5-CF.sub.3                                                                              S      H         O   H, H                                   4-CF.sub.3                                                                               H        S      Me        O   H, H                                   4-Cl      H        S      Me        O   H, H                                   4-Br      H        S      Me        O   H, H                                   4-CF.sub.3                                                                               5-Cl     S      Me        O   H, H                                   4-Cl      5-Cl     S      Me        O   H, H                                   4-Br      5-Cl     S      Me        O   H, H                                   4-CF.sub.3                                                                               5-Br     S      Me        O   H, H                                   4-Cl      5-Br     S      Me        O   H, H                                   4-Br      5-Br     S      Me        O   H, H                                   4-CF.sub.3                                                                               5-CF.sub.3                                                                              S      Me        O   H, H                                   4-Cl      5-CF.sub.3                                                                              S      Me        O   H, H                                   4-Br      5-CF.sub.3                                                                              S      Me        O   H, H                                   4-CF.sub.3                                                                               5-F      S      Me        O   H, H                                   4-Cl      5-F      S      Me        O   H, H                                   4-Br      5-F      S      Me        O   H, H                                   4-CF.sub.3                                                                               H        S      CO.sub.2 Me                                                                              O   H, H                                   4-Cl      H        S      CO.sub.2 Me                                                                              O   H, H                                   4-Br      H        S      CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               5-Cl     S      CO.sub.2 Me                                                                              O   H, H                                   4-Cl      5-Cl     S      CO.sub.2 Me                                                                              O   H, H                                   4-Br      5-Cl     S      CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               H        S      Ph        O   H, H                                   4-Cl      H        S      Ph        O   H, H                                   4-Br      H        S      Ph        O   H, H                                   4-CF.sub.3                                                                               5-Br     S      Ph        O   H, H                                   4-Cl      5-Br     S      Ph        O   H, H                                   4-Br      5-Br     S      Ph        O   H, H                                   4-CF.sub.3                                                                               H        S      H         O   Me,                                                                            Me                                     4-Cl      H        S      H         O   Me,                                                                            Me                                     4-Br      H        S      H         O   Me,                                                                            Me                                     4-CF.sub.3                                                                               H        S      H         O   H, Me                                  4-Cl      H        S      H         O   H, Me                                  4-Br      H        S      H         O   H, Me                                  4-CF.sub.3                                                                               H        S      H         O   H, Ph                                  4-Cl      H        S      H         O   H, Ph                                  4-Br      H        S      H         O   H, Ph                                  4-CF.sub.3                                                                               H        S      H         O   H,                                                                             CO.sub.2 Me                            4-Cl      H        S      H         O   H,                                                                             CO.sub.2 Me                            4-Br      H        S      H         O   H,                                                                             CO.sub.2 Me                            4-CF.sub.3                                                                               H        S      H         S   H, H                                   4-Cl      H        S      H         S   H, H                                   4-Br      H        S      H         S   H, H                                   4-SMe     H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-SO.sub.2 Me                                                                            H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-OCF.sub.2 CF.sub.2 H                                                                   H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.2 Cl                                                                            H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CO.sub.2 Me                                                                            H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CO.sub.2 CF.sub.3                                                                      H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-F       H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CN      H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-Me      H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   3,4-      H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   CH.sub.2 C(Me).sub.2 O.sup.1                                                   3,4-CF.sub.2 CF.sub.2 O.sup.2                                                            H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3, 3-Cl                                                                         H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-I       H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-OMe     H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-O-t-Bu  H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-t-Bu    H        CH.sub.2                                                                              CO.sub.2 Me                                                                              O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 H                                                                               O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CONH.sub.2                                                                               O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CONHMe    O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CONMe     O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 Ph                                                                     O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CH.sub.2 Ph                                                                              O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              OH        O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              OAc       O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.3                                                                              CH.sub.2 CF.sub.3                                                                        O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CH.sub.2 OCH.sub.3                                                                       O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CH.sub.2 CO.sub.2 Me                                                                     O   H, H                                   4-CF.sub.3                                                                               H        CH.sub.2                                                                              CH.sub.2 CH.sub.2 CN                                                                     O   H, H                                   ______________________________________                                          ##STR32##                                                                      ##STR33##                                                                     ?                                                                         

                  TABLE 2                                                          ______________________________________                                         R.sub.1                                                                               R.sub.2  A      B          X   R.sub.a.sup.1, R.sub.a.sup.2             ______________________________________                                         4-CF.sub.3                                                                            H        CH.sub.2                                                                              H          O   H,H                                      4-Cl   H        CH.sub.2                                                                              H          O   H,H                                      4-Br   H        CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              H          O   H,H                                      4-Cl   4-F      CH.sub.2                                                                              H          O   H,H                                      4-Br   4-F      CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            4-Cl     CH.sub.2                                                                              H          O   H,H                                      4-Cl   4-Cl     CH.sub.2                                                                              H          O   H,H                                      4-Br   4-Cl     CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            4-Me     CH.sub.2                                                                              H          O   H,H                                      4-Cl   4-Me     CH.sub.2                                                                              H          O   H,H                                      4-Br   4-Me     CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            4-OMe    CH.sub.2                                                                              H          O   H,H                                      4-Cl   4-OMe    CH.sub.2                                                                              H          O   H,H                                      4-Br   4-OMe    CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            4-Br     CH.sub.2                                                                              H          O   H,H                                      4-Cl   4-Br     CH.sub.2                                                                              H          O   H,H                                      4-Br   4-Br     CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            6-F      CH.sub.2                                                                              H          O   H,H                                      4-Cl   6-F      CH.sub.2                                                                              H          O   H,H                                      4-Br   6-F      CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            6-Cl     CH.sub.2                                                                              H          O   H,H                                      4-Cl   6-Cl     CH.sub.2                                                                              H          O   H,H                                      4-Br   6-Cl     CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            7-F      CH.sub.2                                                                              H          O   H,H                                      4-Cl   7-F      CH.sub.2                                                                              H          O   H,H                                      4-Br   7-F      CH.sub.2                                                                              H          O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              Me         O   H,H                                      4-Cl   H        CH.sub.2                                                                              Me         O   H,H                                      4-Br   H        CH.sub.2                                                                              Me         O   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              CH.sub.3   O   H,H                                      4-Cl   4-F      CH.sub.2                                                                              CH.sub.3   O   H,H                                      4-Br   4-F      CH.sub.2                                                                              CH.sub.3   O   H,H                                      4-CF.sub.3                                                                            4-Cl     CH.sub.2                                                                              CH.sub.3   O   H,H                                      4-Cl   4-Cl     CH.sub.2                                                                              CH.sub.3   O   H,H                                      4-Br   4-Cl     CH.sub.2                                                                              CH.sub.3   O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              Et         O   H,H                                      4-Cl   H        CH.sub.2                                                                              Et         O   H,H                                      4-Br   H        CH.sub.2                                                                              Et         O   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              Et         O   H,H                                      4-Cl   4-F      CH.sub.2                                                                              Et         O   H,H                                      4-Br   4-F      CH.sub.2                                                                              Et         O   H,H                                      4-CF.sub.3                                                                            4-Cl     CH.sub.2                                                                              Et         O   H,H                                      4-Cl   4-Cl     CH.sub.2                                                                              Et         O   H,H                                      4-Br   4-Cl     CH.sub.2                                                                              CH.sub.2   O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              allyl      O   H,H                                      4-Cl   H        CH.sub.2                                                                              allyl      O   H,H                                      4-Br   H        CH.sub.2                                                                              allyl      O   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              allyl      O   H,H                                      4-Cl   4-F      CH.sub. 2                                                                             allyl      O   H,H                                      4-Br   4-F      CH.sub.2                                                                              allyl      O   H,H                                      4-CF.sub.3                                                                            4-Cl     CH.sub.2                                                                              allyl      O   H,H                                      4-Cl   4-Cl     CH.sub.2                                                                              allyl      O   H,H                                      4-Br   4-Cl     CH.sub.2                                                                              allyl      O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Cl   H        CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Br   H        CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Cl   4-F      CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Br   4-F      CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            4-Cl     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Cl   4-Cl     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Br   4-Cl     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            4-CN     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Cl   4-CN     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Br   4-CN     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            4-Br     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Cl   4-Br     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Br   4-Br     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            4-CF.sub.3                                                                              CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Cl   4-CF.sub.3                                                                              CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Br   4-CF.sub.3                                                                              CH.sub.2                                                                              CO.sub. 2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            4-Me     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Cl   4-Me     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-Br   4-Me     CH.sub.2                                                                              CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              CO.sub.2 Et                                                                               O   H,H                                      4-Cl   H        CH.sub.2                                                                              CO.sub.2 Et                                                                               O   H,H                                      4-Br   H        CH.sub.2                                                                              CO.sub.2 Et                                                                               O   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              CO.sub.2 Et                                                                               O   H,H                                      4-Cl   4-F      CH.sub.2                                                                              CO.sub.2 Et                                                                               O   H,H                                      4-Br   4-F      CH.sub.2                                                                              CO.sub.2 Et                                                                               O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              CO.sub.2 -i-Pr                                                                            O   H,H                                      4-Cl   H        CH.sub.2                                                                              CO.sub.2 -i-Pr                                                                            O   H,H                                      4-Br   H        CH.sub.2                                                                              CO.sub.2 -i-Pr                                                                            O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CF.sub.3                                                                O   H,H                                      4-Cl   H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CF.sub.3                                                                O   H,H                                      4-Br   H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CF.sub.3                                                                O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              CO.sub.2 allyl                                                                            O   H,H                                      4-Cl   H        CH.sub.2                                                                              CO.sub.2 allyl                                                                            O   H,H                                      4-Br   H        CH.sub.2                                                                              CO.sub.2 allyl                                                                            O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                             O   H,H                                      4-Cl   H        CH.sub.2                                                                              CO.sub. 2 CH.sub.2 CH.sub.2 Cl                                                            O   H,H                                      4-Br   H        CH.sub.2                                                                              CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                             O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              Ph         O   H,H                                      4-Cl   H        CH.sub.2                                                                              Ph         O   H,H                                      4-Br   H        CH.sub.2                                                                              Ph         O   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              Ph         O   H,H                                      4-Cl   4-F      CH.sub.2                                                                              Ph         O   H,H                                      4-Br   4-F      CH.sub.2                                                                              Ph         O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              4-Cl-Ph    O   H,H                                      4-Cl   H        CH.sub.2                                                                              4-Cl-Ph    O   H,H                                      4-Br   H        CH.sub.2                                                                              4-Cl-Ph    O   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              4-Cl-Ph    O   H,H                                      4-Cl   4-F      CH.sub.2                                                                              4-Cl-Ph    O   H,H                                      4-Br   4-F      CH.sub.2                                                                              4-Cl-Ph    O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              4-F-Ph     O   H,H                                      4-Cl   H        CH.sub.2                                                                              4-F-Ph     O   H,H                                      4-Br   H        CH.sub.2                                                                              4-F-Ph     O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              H          O   H,Me                                     4-Cl   H        CH.sub.2                                                                              H          O   H,Me                                     4-Br   H        CH.sub.2                                                                              H          O   H,Me                                     4-CF.sub.3                                                                            H        CH.sub.2                                                                              H          O   Me,Me                                    4-Cl   H        CH.sub.2                                                                              H          O   Me,Me                                    4-Br   H        CH.sub.2                                                                              H          O   Me,Me                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                              H          S   H,H                                      4-Cl   H        CH.sub.2                                                                              H          S   H,H                                      4-Br   H        CH.sub.2                                                                              H          S   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              Me         S   H,H                                      4-Cl   H        CH.sub.2                                                                              Me         S   H,H                                      4-Br   H        CH.sub.2                                                                              Me         S   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              CO.sub.2 Me                                                                               S   H,H                                      4-Cl   H        CH.sub.2                                                                              CO.sub.2 Me                                                                               S   H,H                                      4-Br   H        CH.sub.2                                                                              CO.sub.2 Me                                                                               S   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                              H          S   H,H                                      4-Cl   H        CH.sub.2                                                                              H          S   H,H                                      4-Br   H        CH.sub.2                                                                              H          S   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              Me         S   H,H                                      4-Cl   4-F      CH.sub.2                                                                              Me         S   H,H                                      4-Br   4-F      CH.sub.2                                                                              Me         S   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              CO.sub.2 Me                                                                               S   H,H                                      4-Cl   4-F      CH.sub.2                                                                              CO.sub.2 Me                                                                               S   H,H                                      4-Br   4-F      CH.sub.2                                                                              CO.sub.2 Me                                                                               S   H,H                                      4-CF.sub.3                                                                            4-F      CH.sub.2                                                                              H          S   H,H                                      4-Cl   4-F      CH.sub.2                                                                              H          S   H,H                                      4-Br   4-F      CH.sub.2                                                                              H          S   H,H                                      4-CF.sub.3                                                                            H        O      H          O   H,H                                      4-Cl   H        O      H          O   H,H                                      4-Br   H        O      H          O   H,H                                      4-CF.sub.3                                                                            4-F      O      H          O   H,H                                      4-Cl   4-F      O      H          O   H,H                                      4-Br   4-F      O      H          O   H,H                                      4-CF.sub.3                                                                            4-Cl     O      H          O   H,H                                      4-Cl   4-Cl     O      H          O   H,H                                      4-Br   4-Cl     O      H          O   H,H                                      4-CF.sub.3                                                                            4-Me     O      H          O   H,H                                      4-Cl   4-Me     O      H          O   H,H                                      4-Br   4-Me     O      H          O   H,H                                      4-CF.sub.3                                                                            H        O      Me         O   H,H                                      4-Cl   H        O      Me         O   H,H                                      4-Br   H        O      Me         O   H,H                                      4-CF.sub.3                                                                            4-F      O      Me         O   H,H                                      4-Cl   4-F      O      Me         O   H,H                                      4-Br   4-F      O      Me         O   H,H                                      4-CF.sub.3                                                                            4-Cl     O      Me         O   H,H                                      4-Cl   4-Cl     O      Me         O   H,H                                      4-Br   4-Cl     O      Me         O   H,H                                      4-CF.sub.3                                                                            4-Me     O      Me         O   H,H                                      4-Cl   4-Me     O      Me         O   H,H                                      4-Br   4-Me     O      Me         O   H,H                                      4-CF.sub.3                                                                            4-CF.sub.3                                                                              O      Me         O   H,H                                      4-Cl   4-CF.sub.3                                                                              O      Me         O   H,H                                      4-Br   4-CF.sub.3                                                                              O      Me         O   H,H                                      4-CF.sub.3                                                                            H        O      CO.sub.2 Me                                                                               O   H,H                                      4-Cl   H        O      CO.sub.2 Me                                                                               O   H,H                                      4-Br   H        O      CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            4-F      O      CO.sub.2 Me                                                                               O   H,H                                      4-Cl   4-F      O      CO.sub.2 Me                                                                               O   H,H                                      4-Br   4-F      O      CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            H        O      Ph         O   H,H                                      4-Cl   H        O      Ph         O   H,H                                      4-Br   H        O      Ph         O   H,H                                      4-CF.sub.3                                                                            4-F      O      Ph         O   H,H                                      4-Cl   4-F      O      Ph         O   H,H                                      4-Br   4-F      O      Ph         O   H,H                                      4-CF.sub.3                                                                            H        O      H          O   Me,Me                                    4-Cl   H        O      H          O   Me,Me                                    4-Br   H        O      H          O   Me,Me                                    4-CF.sub.3                                                                            H        O      H          O   H,Me                                     4-Cl   H        O      H          O   H,Me                                     4-Br   H        O      H          O   H,Me                                     4-CF.sub.3                                                                            H        O      H          O   H,Ph                                     4-Cl   H        O      H          O   H,Ph                                     4-Br   H        O      H          O   H,Ph                                     4-CF.sub.3                                                                            H        O      H          O   H,CO.sub.2 Me                            4-Cl   H        O      H          O   H,CO.sub.2 Me                            4-Br   H        O      H          O   H,CO.sub.2 Me                            4-CF.sub.3                                                                            H        O      H          S   H,H                                      4-Cl   H        O      H          S   H,H                                      4-Br   H        O      H          S   H,H                                      4-CF.sub.3                                                                            H        S      H          O   H,H                                      4-Cl   H        S      H          O   H,H                                      4-Br   H        S      H          O   H,H                                      4-CF.sub.3                                                                            4-F      S      H          O   H,H                                      4-Cl   4-F      S      H          O   H,H                                      4-Br   4-F      S      H          O   H,H                                      4-CF.sub.3                                                                            4-Cl     S      H          O   H,H                                      4-Cl   4-Cl     S      H          O   H,H                                      4-Br   4-Cl     S      H          O   H,H                                      4-CF.sub.3                                                                            4-Me     S      H          O   H,H                                      4-Cl   4-Me     S      H          O   H,H                                      4-Br   4-Me     S      H          O   H,H                                      4-CF.sub.3                                                                            H        S      Me         O   H,H                                      4-Cl   H        S      Me         O   H,H                                      4-Br   H        S      Me         O   H,H                                      4-CF.sub. 3                                                                           4-F      S      Me         O   H,H                                      4-Cl   4-F      S      Me         O   H,H                                      4-Br   4-F      S      Me         O   H,H                                      4-CF.sub.3                                                                            4-Cl     S      Me         O   H,H                                      4-Cl   4-Cl     S      Me         O   H,H                                      4-Br   4-Cl     S      Me         O   H,H                                      4-CF.sub.3                                                                            4-Me     S      Me         O   H,H                                      4-Cl   4-Me     S      Me         O   H,H                                      4-Br   4-Me     S      Me         O   H,H                                      4-CF.sub.3                                                                            6-F      S      Me         O   H,H                                      4-Cl   6-F      S      Me         O   H,H                                      4-Br   6-F      S      Me         O   H,H                                      4-CF.sub.3                                                                            H        S      CO.sub.2 Me                                                                               O   H,H                                      4-Cl   H        S      CO.sub.2 Me                                                                               O   H,H                                      4-Br   H        S      CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            4-F      S      CO.sub.2 Me                                                                               O   H,H                                      4-Cl   4-F      S      CO.sub.2 Me                                                                               O   H,H                                      4-Br   4-F      S      CO.sub.2 Me                                                                               O   H,H                                      4-CF.sub.3                                                                            4-Cl     S      Ph         O   H,H                                      4-Cl   4-Cl     S      Ph         O   H,H                                      4-Br   4-Cl     S      Ph         O   H,H                                      4-CF.sub.3                                                                            H        S      Ph         O   H,H                                      4-Cl   H        S      Ph         O   H,H                                      4-Br   H        S      Ph         O   H,H                                      4-CF.sub.3                                                                            H        S      H          O   Me,Me                                    4-Cl   H        S      H          O   Me,Me                                    4-Br   H        S      H          O   Me,Me                                    4-CF.sub.3                                                                            H        S      H          O   H,Me                                     4-Cl   H        S      H          O   H,Me                                     4-Br   H        S      H          O   H,Me                                     4-CF.sub.3                                                                            H        S      H          O   H,Ph                                     4-Cl   H        S      H          O   H,Ph                                     4-Br   H        S      H          O   H,Ph                                     4-CF.sub.3                                                                            H        S      H          O   H,CO.sub.2 Me                            4-Cl   H        S      H          O   H,CO.sub.2 Me                            4-Br   H        S      H          O   H,CO.sub.2 Me                            4-CF.sub.3                                                                            H        S      H          S   H,H                                      4-Cl   H        S      H          S   H,H                                      4-Br   H        S      H          S   H,H                                      ______________________________________                                    

                  TABLE 3                                                          ______________________________________                                         R.sub.1                                                                               R.sub.2  A       B         X   R.sub.a.sup.1, R.sub.a.sup.2             ______________________________________                                         4-CF.sub.3                                                                            H        CH.sub.2                                                                               H         O   H,H                                      4-Cl   H        CH.sub.2                                                                               H         O   H,H                                      4-Br   H        CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               H         O   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               H         O   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            5-F      CH.sub.2                                                                               H         O   H,H                                      4-Cl   5-F      CH.sub.2                                                                               H         O   H,H                                      4-Br   5-F      CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            5-CN     CH.sub.2                                                                               H         O   H,H                                      4-Cl   5-CN     CH.sub.2                                                                               H         O   H,H                                      4-Br   5-CN     CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            5-Br     CH.sub.2                                                                               H         O   H,H                                      4-Cl   5-Br     CH.sub.2                                                                               H         O   H,H                                      4-Br   5-Br     CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            5-Me     CH.sub.2                                                                               H         O   H,H                                      4-Cl   5-Me     CH.sub.2                                                                               H         O   H,H                                      4-Br   5-Me     CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            7-F      CH.sub.2                                                                               H         O   H,H                                      4-Cl   7-F      CH.sub.2                                                                               H         O   H,H                                      4-Br   7-F      CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            5-NMe.sub.2                                                                             CH.sub.2                                                                               H         O   H,H                                      4-Cl   5-NMe.sub.2                                                                             CH.sub.2                                                                               H         O   H,H                                      4-Br   5-NMe.sub.2                                                                             CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            5-CF.sub.3                                                                              CH.sub.2                                                                               H         O   H,H                                      4-Cl   5-CF.sub.3                                                                              CH.sub.2                                                                               H         O   H,H                                      4-Br   5-CF.sub.3                                                                              CH.sub.2                                                                               H         O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               Me        O   H,H                                      4-Cl   H        CH.sub.2                                                                               Me        O   H,H                                      4-Br   H        CH.sub.2                                                                               Me        O   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               Me        O   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               Me        O   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               Me        O   H,H                                      4-CF.sub.3                                                                            5-CF.sub.3                                                                              CH.sub.2                                                                               Me        O   H,H                                      4-Cl   5-CF.sub.3                                                                              CH.sub.2                                                                               Me        O   H,H                                      4-Br   5-CF.sub.3                                                                              CH.sub.2                                                                               Me        O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               Et        O   H,H                                      4-Cl   H        CH.sub.2                                                                               Et        O   H,H                                      4-Br   H        CH.sub.2                                                                               Et        O   H,H                                      4-CF.sub.3                                                                            5-F      CH.sub.2                                                                               Et        O   H,H                                      4-Cl   5-F      CH.sub.2                                                                               Et        O   H,H                                      4-Br   5-F      CH.sub.2                                                                               Et        O   H,H                                      4-CF.sub.3                                                                            5-CN     CH.sub.2                                                                               Et        O   H,H                                      4-Cl   5-CN     CH.sub.2                                                                               Et        O   H,H                                      4-Br   5-CN     CH.sub.2                                                                               Et        O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               allyl     O   H,H                                      4-Cl   H        CH.sub.2                                                                               allyl     O   H,H                                      4-Br   H        CH.sub.2                                                                               allyl     O   H,H                                      4-CF.sub.3                                                                            5-Br     CH.sub.2                                                                               allyl     O   H,H                                      4-Cl   5-Br     CH.sub.2                                                                               allyl     O   H,H                                      4-Br   5-Br     CH.sub.2                                                                               allyl     O   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               allyl     O   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               allyl     O   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               allyl     O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Cl   H        CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Br   H        CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Cl   5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Br   5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            5-Br     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Cl   5-Br     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Br   5-Br     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            5-CN     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Cl   5-CN     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Br   5-CN     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            5-CF.sub.3                                                                              CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Cl   5-CF.sub.3                                                                              CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Br   5-CF.sub.3                                                                              CH.sub. 2                                                                              CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Cl   5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-Br   5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 Et                                                                              O   H,H                                      4-Cl   H        CH.sub.2                                                                               CO.sub.2 Et                                                                              O   H,H                                      4-Br   H        CH.sub.2                                                                               CO.sub.2 Et                                                                              O   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               CO.sub.2 Et                                                                              O   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               CO.sub.2 Et                                                                              O   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               CO.sub.2 Et                                                                              O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 -i-Pr                                                                           O   H,H                                      4-Cl   H        CH.sub.2                                                                               CO.sub.2 -i-Pr                                                                           O   H,H                                      4-Br   H        CH.sub.2                                                                               CO.sub.2 -i-Pr                                                                           O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CF.sub.3                                                               O   H,H                                      4-Cl   H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CF.sub.3                                                               O   H,H                                      4-Br   H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CF.sub.3                                                               O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 allyl                                                                           O   H,H                                      4-Cl   H        CH.sub.2                                                                               CO.sub.2 allyl                                                                           O   H,H                                      4-Br   H        CH.sub.2                                                                               CO.sub.2 allyl                                                                           O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O   H,H                                      4-Cl   H        CH.sub. 2                                                                              CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O   H,H                                      4-Br   H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               Ph        O   H,H                                      4-Cl   H        CH.sub.2                                                                               Ph        O   H,H                                      4-Br   H        CH.sub.2                                                                               Ph        O   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               Ph        O   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               Ph        O   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               Ph        O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               4-Cl--Ph  O   H,H                                      4-Cl   H        CH.sub.2                                                                               4-Cl--Ph  O   H,H                                      4-Br   H        CH.sub.2                                                                               4-Cl--Ph  O   H,H                                      4-CF.sub.3                                                                            5-CF.sub.3                                                                              CH.sub.2                                                                               4-Cl--Ph  O   H,H                                      4-Cl   5-CF.sub.3                                                                              CH.sub.2                                                                               4-Cl--Ph  O   H,H                                      4-Br   5-CF.sub.3                                                                              CH.sub.2                                                                               4-Cl--Ph  O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               4-F--Ph   O   H,H                                      4-Cl   H        CH.sub.2                                                                               4-F--Ph   O   H,H                                      4-Br   H        CH.sub.2                                                                               4-F--Ph   O   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               H         O   H,Me                                     4-Cl   H        CH.sub.2                                                                               H         O   H,Me                                     4-Br   H        CH.sub.2                                                                               H         O   H,Me                                     4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               H         O   Me,Me                                    4-Cl   5-Cl     CH.sub.2                                                                               H         O   Me,Me                                    4-Br   5-Cl     CH.sub.2                                                                               H         O   Me,Me                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               H         S   H,H                                      4-Cl   H        CH.sub. 2                                                                              H         S   H,H                                      4-Br   H        CH.sub.2                                                                               H         S   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               Me        S   H,H                                      4-Cl   H        CH.sub.2                                                                               Me        S   H,H                                      4-Br   H        CH.sub.2                                                                               Me        S   H,H                                      4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 Me                                                                              S   H,H                                      4-Cl   H        CH.sub.2                                                                               CO.sub.2 Me                                                                              S   H,H                                      4-Br   H        CH.sub.2                                                                               CO.sub.2 Me                                                                              S   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               H         S   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               H         S   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               H         S   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               Me        S   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               Me        S   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               Me        S   H,H                                      4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              S   H,H                                      4-Cl   5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              S   H,H                                      4-Br   5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              S   H,H                                      4-CF.sub.3                                                                            5-Me     CH.sub.2                                                                               H         S   H,H                                      4-Cl   5-Me     CH.sub.2                                                                               H         S   H,H                                      4-Br   5-Me     CH.sub.2                                                                               H         S   H,H                                      4-CF.sub.3                                                                            H        O       H         O   H,H                                      4-Cl   H        O       H         O   H,H                                      4-Br   H        O       H         O   H,H                                      4-CF.sub.3                                                                            5-Cl     O       H         O   H,H                                      4-Cl   5-Cl     O       H         O   H,H                                      4-Br   5-Cl     O       H         O   H,H                                      4-CF.sub.3                                                                            5-Br     O       H         O   H,H                                      4-Cl   5-Br     O       H         O   H,H                                      4-Br   5-Br     O       H         O   H,H                                      4-CF.sub.3                                                                            5-CF.sub.3                                                                              O       H         O   H,H                                      4-Cl   5-CF.sub.3                                                                              O       H         O   H,H                                      4-Br   5-CF.sub.3                                                                              O       H         O   H,H                                      4-CF.sub.3                                                                            H        O       Me        O   H,H                                      4-Cl   H        O       Me        O   H,H                                      4-Br   H        O       Me        O   H,H                                      4-CF.sub.3                                                                            5-Cl     O       Me        O   H,H                                      4-Cl   5-Cl     O       Me        O   H,H                                      4-Br   5-Cl     O       Me        O   H,H                                      4-CF.sub.3                                                                            5-Br     O       Me        O   H,H                                      4-Cl   5-Br     O       Me        O   H,H                                      4-Br   5-Br     O       Me        O   H,H                                      4-CF.sub.3                                                                            5-CF.sub.3                                                                              O       Me        O   H,H                                      4-Cl   5-CF.sub.3                                                                              O       Me        O   H,H                                      4-Br   5-CF.sub.3                                                                              O       Me        O   H,H                                      4-CF.sub.3                                                                            5-F      O       Me        O   H,H                                      4-Cl   5-F      O       Me        O   H,H                                      4-Br   5-F      O       Me        O   H,H                                      4-CF.sub.3                                                                            H        O       CO.sub.2 Me                                                                              O   H,H                                      4-Cl   H        O       CO.sub.2 Me                                                                              O   H,H                                      4-Br   H        O       CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            5-Cl     O       CO.sub.2 Me                                                                              O   H,H                                      4-Cl   5-Cl     O       CO.sub.2 Me                                                                              O   H,H                                      4-Br   5-Cl     O       CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            H        O       Ph        O   H,H                                      4-Cl   H        O       Ph        O   H,H                                      4-Br   H        O       Ph        O   H,H                                      4-CF.sub.3                                                                            5-Br     O       Ph        O   H,H                                      4-Cl   5-Br     O       Ph        O   H,H                                      4-Br   5-Br     O       Ph        O   H,H                                      4-CF.sub.3                                                                            H        O       H         O   Me,Me                                    4-Cl   H        O       H         O   Me,Me                                    4-Br   H        O       H         O   Me,Me                                    4-CF.sub.3                                                                            H        O       H         O   H,Me                                     4-Cl   H        O       H         O   H,Me                                     4-Br   H        O       H         O   H,Me                                     4-CF.sub.3                                                                            H        O       H         O   H,Ph                                     4-Cl   H        O       H         O   H,Ph                                     4-Br   H        O       H         O   H,Ph                                     4-CF.sub.3                                                                            H        O       H         O   H,CO.sub.2 Me                            4-Cl   H        O       H         O   H,CO.sub.2 Me                            4-Br   H        O       H         O   H,CO.sub.2 Me                            4-CF.sub.3                                                                            H        O       H         S   H,H                                      4-Cl   H        O       H         S   H,H                                      4-Br   H        O       H         S   H,H                                      4-CF.sub.3                                                                            H        S       H         O   H,H                                      4-Cl   H        S       H         O   H,H                                      4-Br   H        S       H         O   H,H                                      4-CF.sub.3                                                                            5-Cl     S       H         O   H,H                                      4-Cl   5-Cl     S       H         O   H,H                                      4-Br   5-Cl     S       H         O   H,H                                      4-CF.sub.3                                                                            5-Br     S       H         O   H,H                                      4-Cl   5-Br     S       H         O   H,H                                      4-Br   5-Br     S       H         O   H,H                                      4-CF.sub.3                                                                            5-CF.sub.3                                                                              S       H         O   H,H                                      4-Cl   5-CF.sub.3                                                                              S       H         O   H,H                                      4-Br   5-CF.sub.3                                                                              S       H         O   H,H                                      4-CF.sub.3                                                                            H        S       Me        O   H,H                                      4-Cl   H        S       Me        O   H,H                                      4-Br   H        S       Me        O   H,H                                      4-CF.sub.3                                                                            5-Cl     S       Me        O   H,H                                      4-Cl   5-Cl     S       Me        O   H,H                                      4-Br   5-Cl     S       Me        O   H,H                                      4-CF.sub.3                                                                            5-Br     S       Me        O   H,H                                      4-Cl   5-Br     S       Me        O   H,H                                      4-Br   5-Br     S       Me        O   H,H                                      4-CF.sub.3                                                                            5-CF.sub.3                                                                              S       Me        O   H,H                                      4-Cl   5-CF.sub.3                                                                              S       Me        O   H,H                                      4-Br   5-CF.sub.3                                                                              S       Me        O   H,H                                      4-CF.sub.3                                                                            5-F      S       Me        O   H,H                                      4-Cl   5-F      S       Me        O   H,H                                      4-Br   5-F      S       Me        O   H,H                                      4-CF.sub.3                                                                            H        S       CO.sub.2 Me                                                                              O   H,H                                      4-Cl   H        S       CO.sub.2 Me                                                                              O   H,H                                      4-Br   H        S       CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            5-Cl     S       CO.sub.2 Me                                                                              O   H,H                                      4-Cl   5-Cl     S       CO.sub.2 Me                                                                              O   H,H                                      4-Br   5-Cl     S       CO.sub.2 Me                                                                              O   H,H                                      4-CF.sub.3                                                                            H        S       Ph        O   H,H                                      4-Cl   H        S       Ph        O   H,H                                      4-Br   H        S       Ph        O   H,H                                      4-CF.sub.3                                                                            5-Br     S       Ph        O   H,H                                      4-Cl   5-Br     S       Ph        O   H,H                                      4-Br   5-Br     S       Ph        O   H,H                                      4-CF.sub.3                                                                            H        S       H         O   Me,Me                                    4-Cl   H        S       H         O   Me,Me                                    4-Br   H        S       H         O   Me,Me                                    4-CF.sub.3                                                                            H        S       H         O   H,Me                                     4-Cl   H        S       H         O   H,Me                                     4-Br   H        S       H         O   H,Me                                     4-CF.sub.3                                                                            H        S       H         O   H,Ph                                     4-Cl   H        S       H         O   H,Ph                                     4-Br   H        S       H         O   H,Ph                                     4-CF.sub.3                                                                            H        S       H         O   H,CO.sub.2 Me                            4-Cl   H        S       H         O   H,CO.sub.2 Me                            4-Br   H        S       H         O   H,CO.sub.2 Me                            4-CF.sub.3                                                                            H        S       H         S   H,H                                      4-Cl   H        S       H         S   H,H                                      4-Br   H        S       H         S   H,H                                      ______________________________________                                    

                  TABLE 4                                                          ______________________________________                                         R.sub.1                                                                               R.sub.2  A       B         X    R.sub.a.sup.1, R.sub.a.sup.2            ______________________________________                                         4-CF.sub.3                                                                            H        CH.sub.2                                                                               H         O    H, H                                    4-Cl   H        CH.sub.2                                                                               H         O    H, H                                    4-Br   H        CH.sub.2                                                                               H         O    H, H                                    4-CF.sub.3                                                                            4-Me     CH.sub.2                                                                               H         O    M, M                                    4-Cl   4-Me     CH.sub.2                                                                               H         O    H, H                                    4-Br   4-Me     CH.sub.2                                                                               H         O    H, H                                    4-CF.sub.3                                                                            4-F      CH.sub.2                                                                               H         O    H, H                                    4-Cl   4-F      CH.sub.2                                                                               H         O    H, H                                    4-Br   4-F      CH.sub.2                                                                               H         O    H, H                                    4-CF.sub.3                                                                            4-Cl     CH.sub.2                                                                               H         O    H, H                                    4-Cl   4-Cl     CH.sub.2                                                                               H         O    H, H                                    4-Br   4-Cl     CH.sub.2                                                                               H         O    H, H                                    4-CF.sub.3                                                                            5-F      CH.sub.2                                                                               H         O    H, H                                    4-Cl   5-F      CH.sub.2                                                                               H         O    H, H                                    4-Br   5-F      CH.sub.2                                                                               H         O    H, H                                    4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               H         O    H, H                                    4-Cl   5-Cl     CH.sub.2                                                                               H         O    H, H                                    4-Br   5-Cl     CH.sub.2                                                                               H         O    H, H                                    4-CF.sub.3                                                                            5-Me     CH.sub.2                                                                               H         O    H, H                                    4-Cl   5-Me     CH.sub.2                                                                               H         O    H, H                                    4-Br   5-Me     CH.sub. 2                                                                              H         O    H, H                                    4-CF.sub.3                                                                            5-Br     CH.sub.2                                                                               H         O    H, H                                    4-Cl   5-Br     CH.sub.2                                                                               H         O    H, H                                    4-Br   5-Br     CH.sub.2                                                                               H         O    H, H                                    4-CF.sub.3                                                                            5-OMe    CH.sub.2                                                                               H         O    H, H                                    4-Cl   5-OMe    CH.sub.2                                                                               H         O    H, H                                    4-Br   5-OMe    CH.sub.2                                                                               H         O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               Me        O    H, H                                    4-Cl   H        CH.sub.2                                                                               Me        O    H, H                                    4-Br   H        CH.sub.2                                                                               Me        O    H, H                                    4-CF.sub.3                                                                            4-F      CH.sub.2                                                                               Me        O    H, H                                    4-Cl   4-F      CH.sub.2                                                                               Me        O    H, H                                    4-Br   4-F      CH.sub.2                                                                               Me        O    H, H                                    4-CF.sub.3                                                                            5-F      CH.sub.2                                                                               Me        O    H, H                                    4-Cl   5-F      CH.sub.2                                                                               Me        O    H, H                                    4-Br   5-F      CH.sub.2                                                                               Me        O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               Me        O    H, H                                    4-Cl   H        CH.sub.2                                                                               Et        O    H, H                                    4-Br   H        CH.sub.2                                                                               Et        O    H, H                                    4-CF.sub.3                                                                            4-F      CH.sub.2                                                                               Et        O    H, H                                    4-Cl   4-F      CH.sub.2                                                                               Et        O    H, H                                    4-Br   4-F      CH.sub.2                                                                               Et        O    H, H                                    4-CF.sub.3                                                                            4-Cl     CH.sub.2                                                                               Et        O    H, H                                    4-Cl   4-Cl     CH.sub.2                                                                               Et        O    H, H                                    4-Br   4-Cl     CH.sub. 2                                                                              et        O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               allyl     O    H, H                                    4-Cl   H        CH.sub.2                                                                               allyl     O    H, H                                    4-Br   H        CH.sub.2                                                                               allyl     O    H, H                                    4-CF.sub.3                                                                            5-F      CH.sub.2                                                                               allyl     O    H, H                                    4-Cl   5-F      CH.sub.2                                                                               allyl     O    H, H                                    4-Br   5-F      CH.sub.2                                                                               allyl     O    H, H                                    4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               allyl     O    H, H                                    4-Cl   5-Cl     CH.sub.2                                                                               allyl     O    H, H                                    4-Br   5-Cl     CH.sub.2                                                                               allyl     O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Cl   H        CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Br   H        CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Cl   4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Br   4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Cl   4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Br   4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Cl   5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Br   5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Cl   4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Br   4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Cl   5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Br   5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            5-CF.sub.3                                                                              CH.sub.3                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Cl   5-CF.sub.3                                                                              CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Br   5-CF.sub.3                                                                              CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Cl   5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-Br   5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 Et                                                                              O    H, H                                    4-Cl   H        CH.sub.2                                                                               CO.sub.2 Et                                                                              O    H, H                                    4-Br   H        CH.sub.2                                                                               CO.sub.2 Et                                                                              O    H, H                                    4-CF.sub.3                                                                            5-Me     CH.sub.2                                                                               CO.sub.2 Et                                                                              O    H, H                                    4-Cl   5-Me     CH.sub.2                                                                               CO.sub.2 Et                                                                              O    H, H                                    4-Br   5-Me     CH.sub.2                                                                               CO.sub.2 Et                                                                              O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 i-Pr                                                                            O    H, H                                    4-Cl   H        CH.sub.2                                                                               CO.sub.2 i-Pr                                                                            O    H, H                                    4-Br   H        CH.sub.2                                                                               CO.sub.2 i-Pr                                                                            O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CF.sub.3                                                               O    H, H                                    4-Cl   H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CF.sub.3                                                               O    H, H                                    4-Br   H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CF.sub.3                                                               O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 allyl                                                                           O    H, H                                    4-Cl   H        CH.sub.2                                                                               CO.sub.2 allyl                                                                           O    H, H                                    4-Br   H        CH.sub.2                                                                               CO.sub.2 allyl                                                                           O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O    H, H                                    4-Cl   H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O    H, H                                    4-Br   H        CH.sub.2                                                                               CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               Ph        O    H, H                                    4-Cl   H        CH.sub.2                                                                               Ph        O    H, H                                    4-Br   H        CH.sub.2                                                                               Ph        O    H, H                                    4-CF.sub.3                                                                            4-F      CH.sub.2                                                                               Ph        O    H, H                                    4-Cl   4-F      CH.sub.2                                                                               Ph        O    H, H                                    4-Br   4-F      CH.sub.2                                                                               Ph        O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               4-Cl-Ph   O    H, H                                    4-Cl   H        CH.sub. 2                                                                              4-Cl-Ph   O    H, H                                    4-Br   H        CH.sub.2                                                                               4-Cl-Ph   O    H, H                                    4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               4-Cl-Ph   O    H, H                                    4-Cl   5-Cl     CH.sub.2                                                                               4-Cl-Ph   O    H, H                                    4-Br   5-Cl     CH.sub.2                                                                               4-Cl-Ph   O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               4-F-Ph    O    H, H                                    4-Cl   H        CH.sub.2                                                                               4-F-Ph    O    H, H                                    4-Br   H        CH.sub.2                                                                               4-F-Ph    O    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               H         O    H, Me                                   4-Cl   H        CH.sub.2                                                                               H         O    H, Me                                   4-Br   H        CH.sub.2                                                                               H         O    H, Me                                   4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               H         O    Me, Me                                  4-Cl   5-Cl     CH.sub.2                                                                               H         O    Me, Me                                  4-Br   5-Cl     CH.sub.2                                                                               H         O    Me, Me                                  4-CF.sub.3                                                                            H        CH.sub.2                                                                               H         S    H, H                                    4-Cl   H        CH.sub.2                                                                               H         S    H, H                                    4-Br   H        CH.sub.2                                                                               H         S    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               Me        S    H, H                                    4-Cl   H        CH.sub.2                                                                               Me        S    H, H                                    4-Br   H        CH.sub.2                                                                               Me        S    H, H                                    4-CF.sub.3                                                                            H        CH.sub.2                                                                               CO.sub.2 Me                                                                              S    H, H                                    4-Cl   H        CH.sub.2                                                                               CO.sub.2 Me                                                                              S    H, H                                    4-Br   H        CH.sub.2                                                                               CO.sub.2 Me                                                                              S    H, H                                    4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               H         S    H, H                                    4-Cl   5-Cl     CH.sub.2                                                                               H         S    H, H                                    4-Br   5-Cl     CH.sub.2                                                                               H         S    H, H                                    4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               Me        S    H, H                                    4-Cl   5-Cl     CH.sub.2                                                                               Me        S    H, H                                    4-Br   5-Cl     CH.sub.2                                                                               Me        S    H, H                                    4-CF.sub.3                                                                            5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              S    H, H                                    4-Cl   5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              S    H, H                                    4-Br   5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                              S    H, H                                    4-CF.sub.3                                                                            H        O       H         O    H, H                                    4-Cl   H        O       H         O    H, H                                    4-Br   H        O       H         O    H, H                                    4-CF.sub.3                                                                            5-Cl     O       H         O    H, H                                    4-Cl   5-Cl     O       H         O    H, H                                    4-Br   5-Cl     O       H         O    H, H                                    4-CF.sub.3                                                                            4-F      O       H         O    H, H                                    4-Cl   4-F      O       H         O    H, H                                    4-Br   4-F      O       H         O    H, H                                    4-CF.sub.3                                                                            5-CF.sub.3                                                                              O       H         O    H, H                                    4-Cl   5-CF.sub.3                                                                              O       H         O    H, H                                    4-Br   5-CF.sub.3                                                                              O       H         O    H, H                                    4-CF.sub.3                                                                            H        O       Me        O    H, H                                    4-Cl   H        O       Me        O    H, H                                    4-Br   H        O       Me        O    H, H                                    4-CF.sub.3                                                                            4-F      O       Me        O    H, H                                    4-Cl   4-F      O       Me        O    H, H                                    4-Br   4-F      O       Me        O    H, H                                    4-CF.sub.3                                                                            4-Cl     O       Me        O    H, H                                    4-Cl   4-Cl     O       Me        O    H, H                                    4-Br   4-Cl     O       Me        O    H, H                                    4-CF.sub.3                                                                            5-F      O       Me        O    H, H                                    4-Cl   5-F      O       Me        O    H, H                                    4-Br   5-F      O       Me        O    H, H                                    4-CF.sub.3                                                                            5-Cl     O       Me        O    H, H                                    4-Cl   5-Cl     O       Me        O    H, H                                    4-Br   5-Cl     O       Me        O    H, H                                    4-CF.sub.3                                                                            H        O       CO.sub.2 Me                                                                              O    H, H                                    4-Cl   H        O       CO.sub.2 Me                                                                              O    H, H                                    4-Br   H        O       CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            5-Cl     O       CO.sub.2 Me                                                                              O    H, H                                    4-Cl   5-Cl     O       CO.sub.2 Me                                                                              O    H, H                                    4-Br   5-Cl     O       CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            H        O       Ph        O    H, H                                    4-Cl   H        O       Ph        O    H, H                                    4-Br   H        O       Ph        O    H, H                                    4-CF.sub.3                                                                            5-Cl     O       Ph        O    H, H                                    4-Cl   5-Cl     O       Ph        O    H, H                                    4-Br   5-Cl     O       Ph             H, H                                    4-CF.sub.3                                                                            H        O       H         O    Me, Me                                  4-Cl   H        O       H         O    Me, Me                                  4-Br   H        O       H         O    Me, Me                                  4-CF.sub.3                                                                            H        O       H         O    H, Me                                   4-Cl   H        O       H         O    H, Me                                   4-Br   H        O       H         O    H, Me                                   4-CF.sub.3                                                                            H        O       H         O    H, Ph                                   4-Cl   H        O       H         O    H, Ph                                   4-Br   H        O       H         O    H, Ph                                   4-CF.sub.3                                                                            H        O       O         H    H, CO.sub.2 Me                          4-Cl   H        O       H         O    H, CO.sub.2 Me                          4-Br   H        O       H         O    H, CO.sub.2 Me                          4-CF.sub.3                                                                            H        O       H         S    H, H                                    4-Cl   H        O       H         S    H, H                                    4-Br   H        O       H         S    H, H                                    4-CF.sub.3                                                                            H        S       H         O    H, H                                    4-Cl   H        S       H         O    H, H                                    4-Br   H        S       H         O    H, H                                    4-CF.sub.3                                                                            5-Cl     S       H         O    H, H                                    4-Cl   5-Cl     S       H         O    H, H                                    4-Br   5-Cl     S       H         O    H, H                                    4-CF.sub.3                                                                            4-F      S       H         O    H, H                                    4-Cl   4-F      S       H         O    H, H                                    4-Br   4-F      S       H         O    H, H                                    4-CF.sub.3                                                                            5-CF.sub.3                                                                              S       H         O    H, H                                    4-Cl   5-CF.sub.3                                                                              S       H         O    H, H                                    4-Br   5-CF.sub.3                                                                              S       H         O    H, H                                    4-CF.sub.3                                                                            H        S       Me        O    H, H                                    4-Cl   H        S       Me        O    H, H                                    4-Br   H        S       Me        O    H, H                                    4-CF.sub.3                                                                            4-F      S       Me        O    H, H                                    4-Cl   4-F      S       Me        O    H, H                                    4-Br   4-F      S       Me        O    H, H                                    4-CF.sub.3                                                                            4-Cl     S       Me        O    H, H                                    4-Cl   4-Cl     S       Me        O    H, H                                    4-Br   4-Cl     S       Me        O    H, H                                    4-CF.sub.3                                                                            5-F      S       Me        O    H, H                                    4-Cl   5-F      S       Me        O    H, H                                    4-Br   5-F      S       Me        O    H, H                                    4-CF.sub.3                                                                            5-Cl     S       Me        O    H, H                                    4-Cl   5-Cl     S       Me        O    H, H                                    4-Br   5-Cl     S       Me        O    H, H                                    4-CF.sub.3                                                                            H        S       CO.sub.2 Me                                                                              O    H, H                                    4-Cl   H        S       CO.sub.2 Me                                                                              O    H, H                                    4-Br   H        S       CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            5-Cl     S       CO.sub.2 Me                                                                              O    H, H                                    4-Cl   5-Cl     S       CO.sub.2 Me                                                                              O    H, H                                    4-Br   5-Cl     S       CO.sub.2 Me                                                                              O    H, H                                    4-CF.sub.3                                                                            H        S       Ph        O    H, H                                    4-Cl   H        S       Ph        O    H, H                                    4-Br   H        S       Ph        O    H, H                                    4-CF.sub.3                                                                            5-Cl     S       Ph        O    H, H                                    4-Cl   5-Cl     S       Ph        O    H, H                                    4-Br   5-Cl     S       Ph        O    H, H                                    4-CF.sub.3                                                                            H        S       H         O    Me, Me                                  4-Cl   H        S       H         O    Me, Me                                  4-Br   H        S       H         O    Me, Me                                  4-CF.sub.3                                                                            H        S       H         O    H, Me                                   4-Cl   H        S       H         O    H, Me                                   4-Br   H        S       H         O    H, Me                                   4-CF.sub.3                                                                            H        S       H         O    H, Ph                                   4-Cl   H        S       H         O    H, Ph                                   4-Br   H        S       H         O    H, Ph                                   4-CF.sub.3                                                                            H        S       H         O    H, CO.sub.2 Me                          4-Cl   H        S       H         O    H, CO.sub.2 Me                          4-Br   H        S       H         O    H, CO.sub.2 Me                          4-CF.sub.3                                                                            H        S       H         S    H, H                                    4-Cl   H        S       H         S    H, H                                    4-Br   H        S       H         S    H,H                                     ______________________________________                                    

                  TABLE 5                                                          ______________________________________                                         4-CF.sub.3                                                                               H         CH.sub.2                                                                               H       O   H,H                                    4-Cl      H         CH.sub.2                                                                               H       O   H,H                                    4-Br      H         CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               H       O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               H       O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               5-F       CH.sub.2                                                                               H       O   H,H                                    4-Cl      5-F       CH.sub.2                                                                               H       O   H,H                                    4-Br      5-F       CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               5-Me      CH.sub.2                                                                               H       O   H,H                                    4-Cl      5-Me      CH.sub.2                                                                               H       O   H,H                                    4-Br      5-Me      CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               Me      O   H,H                                    4-Cl      H         CH.sub.2                                                                               Me      O   H,H                                    4-Br      H         CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               5-F       CH.sub.2                                                                               Me      O   H,H                                    4-Cl      5-F       CH.sub.2                                                                               Me      O   H,H                                    4-Br      5-F       CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               5-Me      CH.sub.2                                                                               Me      O   H,H                                    4-Cl      5-Me      CH.sub.2                                                                               Me      O   H,H                                    4-Br      5-Me      CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               Et      O   H,H                                    4-Cl      H         CH.sub.2                                                                               Et      O   H,H                                    4-Br      H         CH.sub.2                                                                               Et      O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               5-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O                                          4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               5-Me      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-Me      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-Me      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               Ph      O   H,H                                    4-Cl      H         CH.sub.2                                                                               Ph      O   H,H                                    4-Br      H         CH.sub.2                                                                               Ph      O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               Ph      O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               Ph      O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               Ph      O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-Cl      H         CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-Br      H         CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-CF.sub.3                                                                               5-CO.sub.2 Me                                                                            CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               H         O       H       O   H,H                                    4-CF.sub.3                                                                               H         O       Me      O   H,H                                    4-CF.sub.3                                                                               H         O       i-Pr    O   H,H                                    4-CF.sub.3                                                                               H         O       CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               H         O       Ph      O   H,H                                    4-CF.sub.3                                                                               H         O       4-F--Ph O   H,H                                    4-CF.sub.3                                                                               H         O       4-Cl--Ph                                                                               O   H,H                                    4-CF.sub.3                                                                               5-F       O       H       O   H,H                                    4-CF.sub.3                                                                               5-F       O       Me      O   H,H                                    4-CF.sub.3                                                                               5-F       O       i-Pr    O   H,H                                    4-CF.sub.3                                                                               5-F       O       CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               5-F       O       Ph      O   H,H                                    4-CF.sub.3                                                                               5-F       O       4-F--Ph O   H,H                                    4-CF.sub.3                                                                               5-F       O       4-Cl--Ph                                                                               O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       H       O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       Me      O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       i-Pr    O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       Ph      O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       4-F--Ph O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       4-Cl--Ph                                                                               O   H,H                                    4-OCF.sub.3                                                                              H         O       H       O   H,H                                    4-OCF.sub.3                                                                              H         O       Me      O   H,H                                    4-OCF.sub.3                                                                              H         O       i-Pr    O   H,H                                    4-OCF.sub.3                                                                              H         O       CO.sub.2 Me                                                                            O   H,H                                    4-OCF.sub.3                                                                              H         O       Ph      O   H,H                                    4-OCF.sub.3                                                                              H         O       4-F--Ph O   H,H                                    4-OCF.sub.3                                                                              H         O       4-Cl--Ph                                                                               O   H,H                                    4-OCF.sub.3                                                                              5-F       O       H       O   H,H                                    4-OCF.sub.3                                                                              5-F       O       Me      O   H,H                                    4-OCF.sub.3                                                                              5-F       O       i-Pr    O   H,H                                    4-OCF.sub.3                                                                              5-F       O       CO.sub.2 Me                                                                            O   H,H                                    4-OCF.sub.3                                                                              5-F       O       Ph      O   H,H                                    4-OCF.sub.3                                                                              5-F       O       4-F--Ph O   H,H                                    4-OCF.sub.3                                                                              5-F       O       4-Cl--Ph                                                                               O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       H       O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       Me      O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       i-Pr    O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       CO.sub.2 Me                                                                            O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       Ph      O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       4-F--Ph O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       4-Cl--Ph                                                                               O   H,H                                    4-Br      H         O       H       O   H,H                                    4-Br      H         O       Me      O   H,H                                    4-Br      H         O       i-Pr    O   H,H                                    4-Br      H         O       CO.sub.2 Me                                                                            O   H,H                                    4-Br      H         O       Ph      O   H,H                                    4-Br      H         O       4-F--Ph O   H,H                                    4-Br      H         O       4-Cl--Ph                                                                               O   H,H                                    4-Br      5-F       O       H       O   H,H                                    4-Br      5-F       O       Me      O   H,H                                    4-Br      5-F       O       i-Pr    O   H,H                                    4-Br      5-F       O       CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-F       O       Ph      O   H,H                                    4-Br      5-F       O       4-F--Ph O   H,H                                    4-Br      5-F       O       4-Cl--Ph                                                                               O   H,H                                    4-Br      5-Cl      O       H       O   H,H                                    4-Br      5-Cl      O       Me      O   H,H                                    4-Br      5-Cl      O       i-Pr    O   H,H                                    4-Br      5-Cl      O       CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-Cl      O       Ph      O   H,H                                    4-Br      5-Cl      O       4-F--Ph O   H,H                                    4-Br      5-Cl      O       4-Cl--Ph                                                                               O   H,H                                    4-Cl      H         O       H       O   H,H                                    4-Cl      H         O       Me      O   H,H                                    4-Cl      H         O       i-Pr    O   H,H                                    4-Cl      H         O       CO.sub.2 Me                                                                            O   H,H                                    4-Cl      H         O       Ph      O   H,H                                    4-Cl      H         O       4-F--Ph O   H,H                                    4-Cl      H         O       4-Cl--Ph                                                                               O   H,H                                    4-Cl      5-F       O       H       O   H,H                                    4-Cl      5-F       O       Me      O   H,H                                    4-Cl      5-F       O       i-Pr    O   H,H                                    4-Cl      5-F       O       CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-F       O       Ph      O   H,H                                    4-Cl      5-F       O       4-F--Ph O   H,H                                    4-Cl      5-F       O       4-Cl--Ph                                                                               O   H,H                                    4-Cl      5-Cl      O       H       O   H,H                                    4-Cl      5-Cl      O       Me      O   H,H                                    4-Cl      5-Cl      O       i-Pr    O   H,H                                    4-Cl      5-Cl      O       CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-Cl      O       Ph      O   H,H                                    4-Cl      5-Cl      O       4-F--Ph O   H,H                                    4-Cl      5-Cl      O       4-Cl--Ph                                                                               O   H,H                                    ______________________________________                                    

                  TABLE 6                                                          ______________________________________                                         R.sub.1   R.sub.2   A       B       X   R.sub.a.sup.1, R.sub.a.sup.2           ______________________________________                                         4-CF.sub.3                                                                               H         CH.sub.2                                                                               H       O   H,H                                    4-Cl      H         CH.sub.2                                                                               H       O   H,H                                    4-Br      H         CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               4-F       CH.sub.2                                                                               H       O   H,H                                    4-Cl      4-F       CH.sub.2                                                                               H       O   H,H                                    4-Br      4-F       CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               4-Cl      CH.sub.2                                                                               H       O   H,H                                    4-Cl      4-Cl      CH.sub.2                                                                               H       O   H,H                                    4-Br      4-Cl      CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               4-Me      CH.sub.2                                                                               H       O   H,H                                    4-Cl      4-Me      CH.sub.2                                                                               H       O   H,H                                    4-Br      4-Me      CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               Me      O   H,H                                    4-Cl      H         CH.sub.2                                                                               Me      O   H,H                                    4-Br      H         CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               4-F       CH.sub.2                                                                               Me      O   H,H                                    4-Cl      4-F       CH.sub.2                                                                               Me      O   H,H                                    4-Br      4-F       CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               4-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-Cl      4-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-Br      4-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               Et      O   H,H                                    4-Cl      H         CH.sub.2                                                                               Et      O   H,H                                    4-Br      H         CH.sub.2                                                                               Et      O   H,H                                    4-CF.sub.3                                                                               4-F       CH.sub.2                                                                               Et      O   H,H                                    4-Cl      4-F       CH.sub.2                                                                               Et      O   H,H                                    4-Br      4-F       CH.sub.2                                                                               Et      O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               4-F       CH.sub.2                                                                               CO.sub.2 Me                                        4-Cl      4-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      4-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               4-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      4-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      4-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               4-Me      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      4-Me      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      4-Me      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H,                                   4-CF.sub.3                                                                               H         CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                    4-Cl      H         CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                    4-Br      H         CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                    4-CF.sub.3                                                                               4-Cl      CH.sub.2                                                                               Ph      O   H,H                                    4-Cl      4-Cl      CH.sub.2                                                                               Ph      O   H,H                                    4-Br      4-Cl      CH.sub.2                                                                               Ph      O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               Ph      O   H,H                                    4-Cl      H         CH.sub. 2                                                                              Ph      O   H,H                                    4-Br      H         CH.sub.2                                                                               Ph      O   H,H                                    4-CF.sub.3                                                                               4-Cl      CH.sub.2                                                                               4-F--Ph O   H,H                                    4-Cl      4-Cl      CH.sub.2                                                                               4-F--Ph O   H,H                                    4-Br      4-Cl      CH.sub.2                                                                               4-F--Ph O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               4-F--Ph O   H,H                                    4-Cl      H         CH.sub.2                                                                               4-F--Ph O   H,H                                    4-Br      H         CH.sub.2                                                                               4-F--Ph O   H,H                                    ______________________________________                                    

                  TABLE 7                                                          ______________________________________                                         R.sub.1   R.sub.2   A       B       X   R.sub.a.sup.1, R.sub.a.sup.2           ______________________________________                                         4-CF.sub.3                                                                               H         CH.sub.2                                                                               H       O   H,H                                    4-Cl      H         CH.sub.2                                                                               H       O   H,H                                    4-Br      H         CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               4-F       CH.sub.2                                                                               H       O   H,H                                    4-Cl      4-F       CH.sub.2                                                                               H       O   H,H                                    4-Br      4-F       CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               H       O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               H       O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               5-F       CH.sub.2                                                                               H       O   H,H                                    4-Cl      5-F       CH.sub.2                                                                               H       O   H,H                                    4-Br      5-F       CH.sub.2                                                                               H       O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               Me      O   H,H                                    4-Cl      H         CH.sub.2                                                                               Me      O   H,H                                    4-Br      H         CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               4-F       CH.sub.2                                                                               Me      O   H,H                                    4-Cl      4-F       CH.sub.2                                                                               Me      O   H,H                                    4-Br      4-F       CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               4-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-Cl      4-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-Br      4-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               5-F       CH.sub.2                                                                               Me      O   H,H                                    4-Cl      5-F       CH.sub.2                                                                               Me      O   H,H                                    4-Br      5-F       CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               Me      O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      H         CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               4-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      4-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      4-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               4-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      4-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      4-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               5-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-F       CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               H         CH.sub.2                                                                               Ph      O   H,H                                    4-Cl      H         CH.sub.2                                                                               Ph      O   H,H                                    4-Br      H         CH.sub.2                                                                               Ph      O   H,H                                    4-CF.sub.3                                                                               4-F       CH.sub.2                                                                               4-F--Ph O   H,H                                    4-Cl      4-F       CH.sub.2                                                                               4-F--Ph O   H,H                                    4-Br      4-F       CH.sub.2                                                                               4-F--Ph O   H,H                                    4-CF.sub.3                                                                               5-Cl      CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-Cl      5-Cl      CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-Br      5-Cl      CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-CF.sub.3                                                                               5-F       CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-Cl      5-F       CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-Br      5-F       CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                    4-CF.sub.3                                                                               H         O       H       O   H,H                                    4-CF.sub.3                                                                               H         O       Me      O   H,H                                    4-CF.sub.3                                                                               H         O       i-Pr    O   H,H                                    4-CF.sub.3                                                                               H         O       CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               H         O       Ph      O   H,H                                    4-CF.sub.3                                                                               H         O       4-F--Ph O   H,H                                    4-CF.sub.3                                                                               H         O       4-Cl--Ph                                                                               O   H,H                                    4-CF.sub.3                                                                               5-F       O       H       O   H,H                                    4-CF.sub.3                                                                               5-F       O       Me      O   H,H                                    4-CF.sub.3                                                                               5-F       O       i-Pr    O   H,H                                    4-CF.sub.3                                                                               5-F       O       CO.sub.2 Me                                                                            O   H,H                                    4-CF.sub.3                                                                               5-F       O       Ph      O   H,H                                    4-CF.sub.3                                                                               5-F       O       4-F--Ph O   H,H                                    4-CF.sub.3                                                                               5-F       O       4-Cl--Ph                                                                               O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       H       O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       Me      O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       i-Pr    O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       CO.sub. 2 Me                                                                           O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       Ph      O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       4-F--Ph O   H,H                                    4-CF.sub.3                                                                               5-Cl      O       4-Cl--Ph                                                                               O   H,H                                    4-OCF.sub.3                                                                              H         O       H       O   H,H                                    4-OCF.sub.3                                                                              H         O       Me      O   H,H                                    4-OCF.sub.3                                                                              H         O       i-Pr    O   H,H                                    4-OCF.sub.3                                                                              H         O       CO.sub.2 Me                                                                            O   H,H                                    4-OCF.sub.3                                                                              H         O       Ph      O   H,H                                    4-OCF.sub.3                                                                              H         O       4-F--Ph O   H,H                                    4-OCF.sub.3                                                                              H         O       4-Cl--Ph                                                                               O   H,H                                    4-OCF.sub.3                                                                              5-F       O       H       O   H,H                                    4-OCF.sub.3                                                                              5-F       O       Me      O   H,H                                    4-OCF.sub.3                                                                              5-F       O       i-Pr    O   H,H                                    4-OCF.sub.3                                                                              5-F       O       CO.sub.2 Me                                                                            O   H,H                                    4-OCF.sub.3                                                                              5-F       O       Ph      O   H,H                                    4-OCF.sub.3                                                                              5-F       O       4-F--Ph O   H,H                                    4-OCF.sub.3                                                                              5-F       O       4-Cl--Ph                                                                               O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       H       O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       Me      O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       i-Pr    O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       CO.sub.2 Me                                                                            O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       Ph      O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       4-F--Ph O   H,H                                    4-OCF.sub.3                                                                              5-Cl      O       4-Cl--Ph                                                                               O   H,H                                    4-Br      H         O       H       O   H,H                                    4-Br      H         O       Me      O   H,H                                    4-Br      H         O       i-Pr    O   H,H                                    4-Br      H         O       CO.sub.2 Me                                                                            O   H,H                                    4-Br      H         O       Ph      O   H,H                                    4-Br      H         O       4-F--Ph O   H,H                                    4-Br      H         O       4-Cl--Ph                                                                               O   H,H                                    4-Br      5-F       O       H       O   H,H                                    4-Br      5-F       O       Me      O   H,H                                    4-Br      5-F       O       i-Pr    O   H,H                                    4-Br      5-F       O       CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-F       O       Ph      O   H,H                                    4-Br      5-F       O       4-F--Ph O   H,H                                    4-Br      5-F       O       4-Cl--Ph                                                                               O   H,H                                    4-Br      5-Cl      O       H       O   H,H                                    4-Br      5-Cl      O       Me      O   H,H                                    4-Br      5-Cl      O       i-Pr    O   H,H                                    4-Br      5-Cl      O       CO.sub.2 Me                                                                            O   H,H                                    4-Br      5-Cl      O       Ph      O   H,H                                    4-Br      5-Cl      O       4-F--Ph O   H,H                                    4-Br      5-Cl      O       4-Cl--Ph                                                                               O   H,H                                    4-Cl      H         O       H       O   H,H                                    4-Cl      H         O       Me      O   H,H                                    4-Cl      H         O       i-Pr    O   H,H                                    4-Cl      H         O       CO.sub.2 Me                                                                            O   H,H                                    4-Cl      H         O       Ph      O   H,H                                    4-Cl      H         O       4-F--Ph O   H,H                                    4-Cl      H         O       4-Cl--Ph                                                                               O   H,H                                    4-Cl      5-F       O       H       O   H,H                                    4-Cl      5-F       O       Me      O   H,H                                    4-Cl      5-F       O       i-Pr    O   H,H                                    4-Cl      5-F       O       CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-F       O       Ph      O   H,H                                    4-Cl      5-F       O       4-F--Ph O   H,H                                    4-Cl      5-F       O       4-Cl--Ph                                                                               O   H,H                                    4-Cl      5-Cl      O       H       O   H,H                                    4-Cl      5-Cl      O       Me      O   H,H                                    4-Cl      5-Cl      O       i-Pr    O   H,H                                    4-Cl      5-Cl      O       CO.sub.2 Me                                                                            O   H,H                                    4-Cl      5-Cl      O       Ph      O   H,H                                    4-Cl      5-Cl      O       4-F--Ph O   H,H                                    4-Cl      5-Cl      O       4-Cl--Ph                                                                               O   H,H                                    ______________________________________                                    

                  TABLE 8                                                          ______________________________________                                         R.sub.1  R.sub.2  A       B       X   R.sub.a.sup.1, r.sub.a.sup.2             ______________________________________                                         4-CF.sub.3                                                                              H        CH.sub.2                                                                               H       O   H,H                                      4-Cl     H        CH.sub.2                                                                               H       O   H,H                                      4-Br     H        CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               H       O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               H       O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              5-F      CH.sub.2                                                                               H       O   H,H                                      4-Cl     5-F      CH.sub.2                                                                               H       O   H,H                                      4-Br     5-F      CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              5-Me     CH.sub.2                                                                               H       O   H,H                                      4-Cl     5-Me     CH.sub.2                                                                               H       O   H,H                                      4-Br     5-Me     CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               Me      O   H,H                                      4-Cl     H        CH.sub.2                                                                               Me      O   H,H                                      4-Br     H        CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              5-F      CH.sub.2                                                                               Me      O   H,H                                      4-Cl     5-F      CH.sub.2                                                                               Me      O   H,H                                      4-Br     5-F      CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              5-Me     CH.sub.2                                                                               Me      O   H,H                                      4-Cl     5-Me     CH.sub.2                                                                               Me      O   H,H                                      4-Br     5-Me     CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               Et      O   H,H                                      4-Cl     H        CH.sub.2                                                                               Et      O   H,H                                      4-Br     H        CH.sub.2                                                                               Et      O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     5-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               Ph      O   H,H                                      4-Cl     H        CH.sub.2                                                                               Ph      O   H,H                                      4-Br     H        CH.sub.2                                                                               Ph      O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               Ph      O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               Ph      O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               Ph      O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                      4-Cl     H        CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                      4-Br     H        CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                      ______________________________________                                    

                  TABLE 9                                                          ______________________________________                                         R.sub.1  R.sub.2  A       B       X   R.sub.a.sup.1, R.sub.a.sup.2             ______________________________________                                         4-CF.sub.3                                                                              H        CH.sub.2                                                                               H       O   H,H                                      4-Cl     H        CH.sub.2                                                                               H       O   H,H                                      4-Br     H        CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              4-F      CH.sub.2                                                                               H       O   H,H                                      4-Cl     4-F      CH.sub.2                                                                               H       O   H,H                                      4-Br     4-F      CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              4-Cl     CH.sub.2                                                                               H       O   H,H                                      4-Cl     4-Cl     CH.sub.2                                                                               H       O   H,H                                      4-Br     4-Cl     CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              4-Me     CH.sub.2                                                                               H       O   H,H                                      4-Cl     4-Me     CH.sub.2                                                                               H       O   H,H                                      4-Br     4-Me     CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               Me      O   H,H                                      4-Cl     H        CH.sub.2                                                                               Me      O   H,H                                      4-Br     H        CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              4-F      CH.sub.2                                                                               Me      O   H,H                                      4-Cl     4-F      CH.sub.2                                                                               Me      O   H,H                                      4-Br     4-F      CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              4-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-Cl     4-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-Br     4-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               Et      O   H,H                                      4-Cl     H        CH.sub.2                                                                               Et      O   H,H                                      4-Br     H        CH.sub.2                                                                               Et      O   H,H                                      4-CF.sub.3                                                                              4-F      CH.sub.2                                                                               Et      O   H,H                                      4-Cl     4-F      CH.sub.2                                                                               Et      O   H,H                                      4-Br     4-F      CH.sub.2                                                                               Et      O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              4-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     4-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     4-Me     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                      5-Cl     H        CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                      4-Br     H        CH.sub.2                                                                               CO.sub.2 Et                                                                            O   H,H                                      4-CF.sub.3                                                                              4-Cl     CH.sub.2                                                                               Ph      O   H,H                                      4-Cl     4-Cl     CH.sub.2                                                                               Ph      O   H,H                                      4-Br     4-Cl     CH.sub.2                                                                               Ph      O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               Ph      O   H,H                                      4-Cl     H        CH.sub.2                                                                               Ph      O   H,H                                      4-Br     H        CH.sub.2                                                                               Ph      O   H,H                                      4-CF.sub.3                                                                              4-Cl     CH.sub.2                                                                               4-F--Ph O   H,H                                      4-Cl     4-Cl     CH.sub.2                                                                               4-F--Ph O   H,H                                      4-Br     4-Cl     CH.sub.2                                                                               4-F--Ph O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               4-F--Ph O   H,H                                      4-Cl     H        CH.sub.2                                                                               4-F--Ph O   H,H                                      4-Br     H        CH.sub.2                                                                               4-F--Ph O   H,H,                                     ______________________________________                                    

                  TABLE 10                                                         ______________________________________                                         R.sub.1  R.sub.2  A       B       X   R.sub.a.sup.1, R.sub.a.sup.2             ______________________________________                                         4-CF.sub.3                                                                              H        CH.sub.2                                                                               H       O   H,H                                      4-Cl     H        CH.sub.2                                                                               H       O   H,H                                      4-Br     H        CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              4-F      CH.sub.2                                                                               H       O   H,H                                      4-Cl     4-F      CH.sub.2                                                                               H       O   H,H                                      4-Br     4-F      CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               H       O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               H       O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              5F       CH.sub.2                                                                               H       O   H,H                                      4-Cl     5-F      CH.sub.2                                                                               H       O   H,H                                      4-Br     5-F      CH.sub.2                                                                               H       O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               Me      O   H,H                                      4-Cl     H        CH.sub.2                                                                               Me      O   H,H                                      4-Br     H        CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              4-F      CH.sub.2                                                                               Me      O   H,H                                      4-Cl     4-F      CH.sub.2                                                                               Me      O   H,H                                      4-Br     4-F      CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              4-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-Cl     4-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-Br     4-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              5-F      CH.sub.2                                                                               Me      O   H,H                                      4-Cl     5-F      CH.sub.2                                                                               Me      O   H,H                                      4-Br     5-F      CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               Me      O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     H        CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     4-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     4-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     5-F      CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               CO.sub.2 Me                                                                            O   H,H                                      4-CF.sub.3                                                                              H        CH.sub.2                                                                               Ph      O   H,H                                      4-Cl     H        CH.sub.2                                                                               Ph      O   H,H                                      4-Br     H        CH.sub.2                                                                               Ph      O   H,H                                      4-CF.sub.3                                                                              4-F      CH.sub.2                                                                               4-F--Ph O   H,H                                      4-Cl     4-F      CH.sub.2                                                                               4-F--Ph O   H,H                                      4-Br     4-F      CH.sub.2                                                                               4-F--Ph O   H,H                                      4-CF.sub.3                                                                              5-Cl     CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                      4-Cl     5-Cl     CH.sub.2                                                                               4-Cl--Ph                                                                               O   H,H                                      4-Br     5-Cl     CH.sub.2                                                                               4-Cl-Ph O   H,H                                      4-CF.sub.3                                                                              5-F      CH.sub.2                                                                               4-Cl-Ph O   H,H                                      4-Cl     5-F      CH.sub.2                                                                               4-Cl-Ph O   H,H                                      4-Br     5-F      CH.sub.2                                                                               4-Cl-Ph O   H,H                                      ______________________________________                                    

                  TABLE 11                                                         ______________________________________                                         R.sub.1                                                                               R.sub.2                                                                               A       B       Q     Y                                          ______________________________________                                         4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-1   Me                                         4-Cl   H      CH.sub.2                                                                               H       Q-1   Me                                         4-Br   H      CH.sub.2                                                                               H       Q-1   Me                                         4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               Me      Q-1   Me                                         4-Cl   5-Cl   CH.sub.2                                                                               Me      Q-1   Me                                         4-Br   5-Cl   CH.sub.2                                                                               Me      Q-1   Me                                         4-CF.sub.3                                                                            H      CH.sub.2                                                                               Me      Q-1   Me                                         4-Cl   H      CH.sub.2                                                                               Me      Q-1   Me                                         4-Br   H      CH.sub.2                                                                               Me      Q-1   Me                                         4-CF.sub.3                                                                            H      CH.sub.2                                                                               Me      Q-1   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               Me      Q-1   C(O)Me                                     4-Br   H      CH.sub.2                                                                               Me      Q-1   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-Cl   H      CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-Br   H      CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               Me      Q-1   Me                                         4-Cl   5-Cl   CH.sub.2                                                                               Me      Q-1   Me                                         4-Br   5-Cl   CH.sub.2                                                                               Me      Q-1   Me                                         4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               Me      Q-1   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               Me      Q-1   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               Me      Q-1   C(O)Me                                     4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-Cl   5-Cl   CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-Br   5-Cl   CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            5-F    CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-Cl   5-F    CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-Br   5-F    CH.sub.2                                                                               Me      Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   C(O)Me                                     4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   Me                                         4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   Me                                         4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   Me                                         4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   CO.sub.2 Me                                4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   CO.sub.2 Me                                4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   C(O)Me                                     4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   CO.sub.2 Me                                4-Cl   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   CO.sub.2 Me                                4-Br   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            H      CH.sub.2                                                                               Ph      Q-1   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               Ph      Q-1   C(O)Me                                     4-Br   H      CH.sub.2                                                                               Ph      Q-1   C(O)Me                                     4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               Ph      Q-1   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               Ph      Q-1   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               Ph      Q-1   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               4-Cl--Ph                                                                               Q-1   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               4-Cl--Ph                                                                               Q-1   C(O)Me                                     4-Br   H      CH.sub.2                                                                               4-Cl--Ph                                                                               Q-1   C(O)Me                                     4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               4-Cl--Ph                                                                               Q-1   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               4-Cl--Ph                                                                               Q-1   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               4-Cl--Ph                                                                               Q-1   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-2   Me                                         4-Cl   H      CH.sub.2                                                                               H       Q-2   Me                                         4-Br   H      CH.sub.2                                                                               H       Q-2   Me                                         4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-2   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               H       Q-2   C(O)Me                                     4-Br   H      CH.sub.2                                                                               H       Q-2   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   Me                                         4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   Me                                         4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   Me                                         4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   C(O)Me                                     4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   CO.sub.2 Me                                4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   CO.sub.2 Me                                4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   CO.sub.2 Me                                4-CF.sub.3                                                                            4-F    CH.sub.2                                                                               H       Q-2   Me                                         4-Cl   4-F    CH.sub.2                                                                               H       Q-2   Me                                         4-Br   4-F    CH.sub.2                                                                               H       Q-2   Me                                         4-CF.sub.3                                                                            4-F    CH.sub.2                                                                               H       Q-2   C(O)Me                                     4-Cl   4-F    CH.sub.2                                                                               H       Q-2   C(O)Me                                     4-Br   4-F    CH.sub.2                                                                               H       Q-2   C(O)Me                                     4-CF.sub.3                                                                            4-F    CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   CO.sub.2 Me                                4-Cl   4-F    CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   CO.sub.2 Me                                4-Br   4-F    CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   CO.sub.2 Me                                4-CF.sub.3                                                                            4-F    CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   C(O)Me                                     4-Cl   4-F    CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   Ac                                         4-Br   4-F    CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-2   Ac                                         4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-3   Me                                         4-Cl   H      CH.sub.2                                                                               H       Q-3   Me                                         4-Br   H      CH.sub.2                                                                               H       Q-3   Ac                                         4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-3   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               H       Q-3   CO.sub.2 Me                                4-Br   H      CH.sub.2                                                                               H       Q-3   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               H       Q-3   Me                                         4-Cl   5-Cl   CH.sub.2                                                                               H       Q-3   Me                                         4-Br   5-Cl   CH.sub.2                                                                               H       Q-3   C(O)Me                                     4-CF.sub.3                                                                            5-Cl   CH.sub. 2                                                                              H       Q-3   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               H       Q-3   CO.sub.2 Me                                4-Br   5-Cl   CH.sub.2                                                                               H       Q-3   CO.sub.2 Me                                4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   Me                                         4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   Me                                         4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   C(O)Me                                     4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   CO.sub.2 Me                                4-Cl   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   CO.sub.2 Me                                4-Br   H      CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   Me                                         4-Cl   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   Me                                         4-Br   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   Me                                         4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-3   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-5   C(O)Me                                     4-Cl   H      CH.sub.2                                                                               H       Q-5   C(O)Me                                     4-Br   H      CH.sub.2                                                                               H       Q-5   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-5   CO.sub.2 Me                                4-Cl   H      CH.sub.2                                                                               H       Q-5   CO.sub.2 Me                                4-Br   H      CH.sub.2                                                                               H       Q-5   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-5   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-5   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-5   C(O)Me                                     4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-5   CO.sub.2 Me                                4-Cl   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-5   CO.sub.2 Me                                4-Br   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-5   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               Me      Q-5   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               Me      Q-5   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               Me      Q-5   C(O)Me                                     4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-5   CO.sub.2 Me                                4-Cl   H      CH.sub.2                                                                               H       Q-7   CO.sub.2 Me                                4-Br   H      CH.sub.2                                                                               H       Q-7   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               H       Q-7   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               H       Q-7   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               H       Q-7   C(O)Me                                     4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-7   CO.sub.2 Me                                4-Cl   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-7   CO.sub.2 Me                                4-Br   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-7   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-7   C(O)Me                                     4-Cl   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-7   C(O)Me                                     4-Br   5-Cl   CH.sub.2                                                                               CO.sub.2 Me                                                                            Q-7   C(O)Me                                     4-CF.sub.3                                                                            H      O       H       Q-1   Me                                         4-Cl   H      O       H       Q-1   C(O)Me                                     4-Br   H      O       H       Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            H      O       Me      Q-1   Me                                         4-Cl   H      O       Me      Q-1   C(O)Me                                     4-Br   H      O       Me      Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            5-Cl   O       H       Q-1   Me                                         4-Cl   5-Cl   O       H       Q-1   C(O)Me                                     4-Br   5-Cl   O       H       Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            H      O       H       Q-2   Me                                         4-Cl   H      O       H       Q-2   C(O)Me                                     4-Br   H      O       H       Q-2   CO.sub.2 Me                                4-CF.sub.3                                                                            H      O       H       Q-2   Me                                         4-Cl   H      O       H       Q-2   C(O)Me                                     4-Br   H      O       H       Q-2   CO.sub.2 Me                                4-CF.sub.3                                                                            H      O       H       Q-3   Me                                         4-Cl   H      O       H       Q-3   C(O)Me                                     4-Br   H      O       H       Q-3   CO.sub.2 Me                                4-CF.sub.3                                                                            H      O       H       Q-3   Me                                         4-Cl   H      O       H       Q-3   C(O)Me                                     4-Br   H      O       H       Q-3   CO.sub.2 Me                                4-CF.sub.3                                                                            H      O       H       Q-5   Me                                         4-Cl   H      O       H       Q-5   C(O)Me                                     4-Br   H      O       H       Q-5   CO.sub.2 Me                                4-CF.sub.3                                                                            H      O       H       Q-5   Me                                         4-Cl   H      O       H       Q-5   C(O)Me                                     4-Br   H      O       H       Q-5   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       H       Q-1   Me                                         4-Cl   H      S       H       Q-1   C(O)Me                                     4-Br   H      S       H       Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       CO.sub.2 Me                                                                            Q-1   Me                                         4-Cl   H      S       CO.sub.2 Me                                                                            Q-1   C(O)Me                                     4-Br   H      S       CO.sub.2 Me                                                                            Q-1   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       H       Q-2   Me                                         4-Cl   H      S       H       Q-2   C(O)Me                                     4-Br   H      S       H       Q-2   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       CO.sub.2 Me                                                                            Q-2   Me                                         4-Cl   H      S       CO.sub.2 Me                                                                            Q-2   C(O)Me                                     4-Br   H      S       CO.sub.2 Me                                                                            Q-2   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       H       Q-3   Me                                         4-Cl   H      S       H       Q-3   C(O)Me                                     4-Br   H      S       H       Q-3   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       CO.sub.2 Me                                                                            Q-3   Me                                         4-Cl   H      S       CO.sub.2 Me                                                                            Q-3   C(O)Me                                     4-Br   H      S       CO.sub.2 Me                                                                            Q-3   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       H       Q-5   Me                                         4-Cl   H      S       H       Q-5   C(O)Me                                     4-Br   H      S       H       Q-5   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       CO.sub.2 Me                                                                            Q-5   Me                                         4-Cl   H      S       CO.sub.2 Me                                                                            Q-5   C(O)Me                                     4-Br   H      S       CO.sub.2 Me                                                                            Q-5   CO.sub.2 Me                                4-CF.sub.3                                                                            H      S       H       Q-7   Me                                         4-Cl   H      S       H       Q-7   C(O)Me                                     4-Br   H      S       H       Q-7   CO.sub.2 Me                                4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-1   N(Me)CO.sub.2 Et                           4-Cl   H      CH.sub.2                                                                               H       Q-1   N(Me)CO.sub.2 Et                           4-Br   H      CH.sub.2                                                                               H       Q-1   N(Me)CO.sub.2 Et                           4-CF.sub.3                                                                            H      CH.sub.2                                                                               H       Q-1   N(Me)CO.sub.2 nBu                          4-Cl   H      CH.sub.2                                                                               H       Q-1   N(Me)CO.sub.2 nBu                          4-Br   H      CH.sub.2                                                                               H       Q-1   N(Me)CO.sub.2 nBu                          ______________________________________                                    

                  TABLE 12                                                         ______________________________________                                         R.sub.1                                                                               R.sub.2                                                                               A      B       Q    J                                            ______________________________________                                         4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-1  N(iPr)CO.sub.2 Et                            4-Cl   5-Cl   CH.sub.2                                                                              H       Q-1  N(iPr)CO.sub.2 Et                            4-Br   5-Cl   CH.sub.2                                                                              H       Q-1  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-1  N(Et)CO.sub.2 Et                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-1  N(Et)CO.sub.2 Et                             4-Br   5-Cl   CH.sub.2                                                                              H       Q-1  N(Et)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Et)CO.sub.2 Et                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Et)CO.sub.2 Et                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Et)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(iPr)CO.sub.2 Et                            4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(iPr)CO.sub.2 Et                            4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(iPr)CO.sub.2 Et                            4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(iPr)CO.sub.2 Et                            4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)CO.sub.2 nHex                           4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)CO.sub.2 nHex                           4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)CO.sub.2 nHex                           4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-1  N(Me)CO.sub.2 Et                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-1  N(Me)CO.sub.2 Et                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-1  N(Me)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-3  N(Me)CO.sub.2 Et                             4-Cl   H      CH.sub.2                                                                              H       Q-3  N(Me)CO.sub.2 Et                             4-Br   H      CH.sub.2                                                                              H       Q-3  N(Me)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-3  N(Me)CO.sub.2 nBu                            4-Cl   H      CH.sub.2                                                                              H       Q-3  N(Me)CO.sub.2 nBu                            4-Br   H      CH.sub.2                                                                              H       Q-3  N(Me)CO.sub.2 nBu                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-3  N(iPr)CO.sub.2 Et                            4-Cl   5-Cl   CH.sub.2                                                                              H       Q-3  N(iPr)CO.sub.2 Et                            4-Br   5-Cl   CH.sub.2                                                                              H       Q-3  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-3  N(Et)CO.sub.2 Et                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-3  N(Et)CO.sub.2 Et                             4-Br   5-Cl   CH.sub.2                                                                              H       Q-3  N(Et)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Et)CO.sub.2 Et                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Et)CO.sub.2 Et                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Et)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(iPr)CO.sub. 2 Et                           4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(iPr)CO.sub.2 Et                            4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(iPr)CO.sub.2 Et                            4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(iPr)CO.sub.2 Et                            4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)CO.sub.2 nHex                           4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)CO.sub.2 nHex                           4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)CO.sub.2 nHex                           4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-3  N(Me)CO.sub.2 Et                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-3  N(Me)CO.sub.2 Et                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-3  N(Me)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-4  N(Me)CO.sub.2 Et                             4-Cl   H      CH.sub.2                                                                              H       Q-4  N(Me)CO.sub.2 Et                             4-Br   H      CH.sub.2                                                                              H       Q-4  N(Me)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-4  N(Me)CO.sub.2 nBu                            4-Cl   H      CH.sub.2                                                                              H       Q-4  N(Me)CO.sub.2 nBu                            4-Br   H      CH.sub.2                                                                              H       Q-4  N(Me)CO.sub.2 nBu                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-4  N(iPr)CO.sub.2 Et                            4-Cl   5-Cl   CH.sub.2                                                                              H       Q-4  N(iPr)CO.sub.2 Et                            4-Br   5-Cl   CH.sub.2                                                                              H       Q-4  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-4  N(Et)CO.sub.2 Et                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-4  N(Et)CO.sub.2 Et                             4-Br   5-Cl   CH.sub.2                                                                              H       Q-4  N(Et)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Et)CO.sub.2 Et                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Et)CO.sub.2 Et                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Et)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(iPr)CO.sub.2 Et                            4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(iPr)CO.sub.2 Et                            4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(iPr)CO.sub.2 Et                            4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(iPr)CO.sub.2 Et                            4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)CO.sub.2 nHex                           4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)CO.sub.2 nHex                           4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)CO.sub.2 nHex                           4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-4  N(Me)CO.sub.2 Et                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-4  N(Me)CO.sub.2 Et                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-4  N(Me)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub. 2                                                                             H       Q-5  N(Me)CO.sub.2 Et                             4-Cl   H      CH.sub.2                                                                              H       Q-5  N(Me)CO.sub.2 Et                             4-Br   H      CH.sub.2                                                                              H       Q-5  N(Me)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-5  N(Me)CO.sub.2 nBu                            4-Cl   H      CH.sub.2                                                                              H       Q-5  N(Me)CO.sub.2 nBu                            4-Br   H      CH.sub.2                                                                              H       Q-5  N(Me)CO.sub.2 nBu                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-5  N(iPr)CO.sub.2 Et                            4-Cl   5-Cl   CH.sub.2                                                                              H       Q-5  N(iPr)CO.sub.2 Et                            4-Br   5-Cl   CH.sub.2                                                                              H       Q-5  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-5  N(Et)CO.sub.2 Et                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-5  N(Et)CO.sub.2 Et                             4-Br   5-Cl   CH.sub.2                                                                              H       Q-5  N(Et)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Et)CO.sub.2 Et                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Et)CO.sub.2 Et                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Et)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(iPr)CO.sub.2 Et                            4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(iPr)CO.sub.2 Et                            4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(iPr)CO.sub.2 Et                            4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(iPr)CO.sub.2 Et                            4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(iPr)CO.sub.2 Et                            4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)CO.sub.2 nHex                           4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)CO.sub.2 nHex                           4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)CO.sub.2 nHex                           4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-5  N(Me)CO.sub.2 Et                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-5  N(Me)CO.sub.2 Et                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-5  N(Me)CO.sub.2 Et                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-1  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Ph      Q-1  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Ph      Q-1  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-1  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Me      Q-1  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Me      Q-1  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-1  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-1  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-1  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Me                             4-Cl   5-Me   CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Me                             4-Br   5-Me   CH.sub.2                                                                              H       Q-1  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Ph-4-Me                        4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Ph-4-Me                        4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  N(Me)SO.sub.2 Ph-4-Me                        4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-2  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              H       Q-2  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              H       Q-2  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-2  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-2  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-2  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-2  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Ph      Q-2  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Ph      Q-2  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-2  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Me      Q-2  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Me      Q-2  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-3  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              H       Q-3  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              H       Q-3  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-3  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Ph      Q-3  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Ph      Q-3  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-3  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Me      Q-3  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Me      Q-3  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-3  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-3  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub. 2                                                                             H       Q-3  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-3  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-3  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-3  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-3  N(Me)SO.sub.2 Me                             4-Cl   5-Me   CH.sub.2                                                                              H       Q-3  N(Me)SO.sub.2 Me                             4-Br   5-Me   CH.sub.2                                                                              H       Q-3  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Ph-4-Me                        4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Ph-4-Me                        4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  N(Me)SO.sub.2 Ph-4-Me                        4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-4  N(Me)SO.sub. 2 Ph                            4-Cl   H      CH.sub.2                                                                              Ph      Q-4  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Ph      Q-4  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-4  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Me      Q-4  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Me      Q-4  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-4  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-4  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-4  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Me                             4-Cl   5-Me   CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Me                             4-Br   5-Me   CH.sub.2                                                                              H       Q-4  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Ph-4-Me                        4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Ph-4-Me                        4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  N(Me)SO.sub.2 Ph-4-Me                        4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-5  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Ph      Q-5  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Ph      Q-5  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-5  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Me      Q-5  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Me      Q-5  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-5  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-5  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-5  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Me                             4-Cl   5-Me   CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Me                             4-Br   5-Me   CH.sub.2                                                                              H       Q-5  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Ph-4-Me                        4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Ph-4-Me                        4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  N(Me)SO.sub.2 Ph-4-Me                        4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-7  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Ph      Q-7  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Ph      Q-7  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-7  N(Me)SO.sub.2 Ph                             4-Cl   H      CH.sub.2                                                                              Me      Q-7  N(Me)SO.sub.2 Ph                             4-Br   H      CH.sub.2                                                                              Me      Q-7  N(Me)SO.sub.2 Ph                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-7  N(Me)SO.sub.2 Me                             4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-7  N(Me)SO.sub.2 Me                             4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-7  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Me                             4-Cl   5-Me   CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Me                             4-Br   5-Me   CH.sub.2                                                                              H       Q-7  N(Me)SO.sub.2 Me                             4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Ph-4-Me                        4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Ph-4-Me                        4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-7  N(Me)SO.sub.2 Ph-4-Me                        4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-1  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              H       Q-1  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              H       Q-1  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub. 2 Me                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-1  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              Ph      Q-1  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              Ph      Q-1  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-1  CO.sub.2 Et                                  4-Cl   H      CH.sub.2                                                                              Me      Q-1  CO.sub.2 Et                                  4-Br   H      CH.sub.2                                                                              Me      Q-1  CO.sub.2 Et                                  4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-1  CO.sub.2 nPr                                 4-Cl   5-Cl   CH.sub.2                                                                              H       Q-1  CO.sub.2 nPr                                 4-Br   5-Cl   CH.sub.2                                                                              H       Q-1  CO.sub.2 nPr                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nPr                                 4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nPr                                 4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nPr                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-1  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-1  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-1  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-1  CO.sub.2 CH.sub.2 Ph                         4-Cl   5-Me   CH.sub.2                                                                              H       Q-1  CO.sub.2 CH.sub.2 Ph                         4-Br   5-Me   CH.sub.2                                                                              H       Q-1  CO.sub.2 CH.sub.2 Ph                         4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub. 2 Me                                                                           Q-1  CO.sub.2 CH.sub.2 Ph                         4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 CH.sub.2 Ph                         4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 CH.sub.2 Ph                         4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-1  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              Ph      Q-1  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              Ph      Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-1  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              Me      Q-1  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              Me      Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-1  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-1  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-Cl   5-Me   CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-Br   5-Me   CH.sub.2                                                                              H       Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-1  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-3  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              H       Q-3  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              H       Q-3  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-3  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              Ph      Q-3  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              Ph      Q-3  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-3  CO.sub.2 Et                                  4-Cl   H      CH.sub.2                                                                              Me      Q-3  CO.sub.2 Et                                  4-Br   H      CH.sub.2                                                                              Me      Q-3  CO.sub.2 Et                                  4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-3  CO.sub.2 nPr                                 4-Cl   5-Cl   CH.sub.2                                                                              H       Q-3  CO.sub.2 nPr                                 4-Br   5-Cl   CH.sub.2                                                                              H       Q-3  CO.sub.2 nPr                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nPr                                 4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nPr                                 4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nPr                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-3  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-3  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-3  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-3  CO.sub.2 CH.sub.2 Ph                         4-Cl   5-Me   CH.sub.2                                                                              H       Q-3  CO.sub.2 CH.sub.2 Ph                         4-Br   5-Me   CH.sub.2                                                                              H       Q-3  CO.sub.2 CH.sub.2 Ph                         4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 CH.sub.2 Ph                         4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 CH.sub.2 Ph                         4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 CH.sub.2 Ph                         4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-3  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              Ph      Q-3  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              Ph      Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-3  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              Me      Q-3  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              Me      Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-3  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-3  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub. 2                                                                             Ph      Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-Cl   5-Me   CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-Br   5-Me   CH.sub.2                                                                              H       Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-3  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-4  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              H       Q-4  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              H       Q-4  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-4  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              Ph      Q-4  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              Ph      Q-4  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-4  CO.sub.2 Et                                  4-Cl   H      CH.sub.2                                                                              Me      Q-4  CO.sub.2 Et                                  4-Br   H      CH.sub.2                                                                              Me      Q-4  CO.sub.2 Et                                  4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-4  CO.sub.2 nPr                                 4-Cl   5-Cl   CH.sub.2                                                                              H       Q-4  CO.sub.2 nPr                                 4-Br   5-Cl   CH.sub.2                                                                              H       Q-4  CO.sub.2 nPr                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nPr                                 4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nPr                                 4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nPr                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-4  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-4  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-4  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-4  CO.sub.2 CH.sub.2 Ph                         4-Cl   5-Me   CH.sub.2                                                                              H       Q-4  CO.sub.2 CH.sub.2 Ph                         4-Br   5-Me   CH.sub.2                                                                              H       Q-4  CO.sub.2 CH.sub.2 Ph                         4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 CH.sub.2 Ph                         4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 CH.sub.2 Ph                         4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 CH.sub.2 Ph                         4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub. 2 nBu                                4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-4  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              Ph      Q-4  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              Ph      Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-4  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              Me      Q-4  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              Me      Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-4  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-4  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-Cl   5-Me   CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-Br   5-Me   CH.sub.2                                                                              H       Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nBu                                 4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nBu                                 4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-4  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-5  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              H       Q-5  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              H       Q-5  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-5  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              Ph      Q-5  CO.sub.2 Me                                  4-Br   H      CH.sub.2                                                                              Ph      Q-5  CO.sub.2 Me                                  4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-5  CO.sub.2 Me                                  4-Cl   H      CH.sub.2                                                                              Me      Q-5  CO.sub.2 Et                                  4-Br   H      CH.sub.2                                                                              Me      Q-5  CO.sub.2 Et                                  4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-5  CO.sub.2 nPr                                 4-Cl   5-Cl   CH.sub.2                                                                              H       Q-5  CO.sub.2 nPr                                 4-Br   5-Cl   CH.sub.2                                                                              H       Q-5  CO.sub.2 nPr                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nPr                                 4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nPr                                 4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nPr                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-5  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-5  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-5  CO.sub.2 CH.sub.2 CH.sub.2 OEt               4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-5  CO.sub.2 CH.sub.2 Ph                         4-Cl   5-Me   CH.sub.2                                                                              H       Q-5  CO.sub.2 CH.sub.2 Ph                         4-Br   5-Me   CH.sub.2                                                                              H       Q-5  CO.sub.2 CH.sub.2 Ph                         4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 CH.sub.2 Ph                         4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 CH.sub.2 Ph                         4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 CH.sub.2 Ph                         4-CF.sub.3                                                                            H      CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Ph      Q-5  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              Ph      Q-5  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              Ph      Q-5  CO.sub.2 nBu                                 4-CF.sub.3                                                                            H      CH.sub.2                                                                              Me      Q-5  CO.sub.2 nBu                                 4-Cl   H      CH.sub.2                                                                              Me      Q-5  CO.sub.2 nBu                                 4-Br   H      CH.sub.2                                                                              Me      Q-5  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Cl   CH.sub.2                                                                              Ph      Q-5  CO.sub.2 nBu                                 4-Cl   5-Cl   CH.sub.2                                                                              Ph      Q-5  CO.sub.2 nBu                                 4-Br   5-Cl   CH.sub.2                                                                              Ph      Q-5  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-Cl   5-Me   CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-Br   5-Me   CH.sub.2                                                                              H       Q-5  CO.sub.2 nBu                                 4-CF.sub.3                                                                            5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 4-Cl   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 4-Br   5-Me   CH.sub.2                                                                              CO.sub.2 Me                                                                            Q-5  CO.sub.2 nBu                                 ______________________________________                                    

                  TABLE 13                                                         ______________________________________                                         R.sub.1     R.sub.2     B             X                                        ______________________________________                                         H           H           H             O                                        4-Cl        H           H             O                                        4-F         H           H             O                                        4-Br        H           H             O                                        4-CF.sub.3  H           H             O                                        4-OCF.sub.2 H                                                                              H           H             O                                        4-CF.sub.3 Cl                                                                              H           H             O                                        4-CO.sub.2 Me                                                                              H           H             O                                        4-CO.sub.2 -i-Pr                                                                           H           H             O                                        4-NO.sub.2  H           H             O                                        4-SMe       H           H             O                                        4-SO.sub.2 Me                                                                              H           H             O                                        4-CF.sub.2 Cl                                                                              H           H             O                                        4-OCF.sub.3 H           H             O                                        4-I         H           H             O                                        4-OCF.sub.2 CF.sub.2 H                                                                     H           H             O                                        4-CN        H           H             O                                        4-Me        H           H             O                                        3,4-CF.sub.2 CF.sub.2 O                                                                    H           H             O                                        3,4-OCF.sub.2 CF.sub.2                                                                     H           H             O                                        3,4-(Me).sub.2 CCH.sub.2 O                                                                 H           O             O                                        4-Cl        H           Me            O                                        4-Br        H           Me            O                                        4-CF.sub.3  H           Me            O                                        4-SMe       H           Me            O                                        4-OCF.sub.2 H                                                                              H           Me            O                                        4-CF.sub.3  H           Et            O                                        4-CO.sub.2 i-Pr                                                                            H           Me            O                                        4-Cl        H           allyl         O                                        4-Br        H           allyl         O                                        4-CF.sub.3  H           allyl         O                                        4-Cl        H           CH.sub.2 Ph   O                                        4-Br        H           CH.sub.2 Ph   O                                        4-CF.sub.3  H           CH.sub.2 Ph   O                                        4-CF.sub.3  H           4-F-CH.sub.2 Ph                                                                              O                                        4-SMe       H           4-F-CH.sub.2 Ph                                                                              O                                        4-CF.sub.3  H           4-F-CH.sub.2 Ph                                                                              O                                        4-CF.sub.3  H           4-Cl-CH.sub.2 Ph                                                                             O                                        4-NO.sub.2  H           4-Cl-CH.sub.2 Ph                                                                             O                                        4-OCF.sub.2 H                                                                              H           Ph            O                                        4-OCF.sub.3 H           Ph            O                                        4-CF.sub.3  H           Ph            O                                        4-Cl        H           4-Cl-Ph       O                                        4-Br        H           4-Cl-Ph       O                                        4-OMe       H           4-Cl-Ph       O                                        4-CF.sub.3  H           n-Bu          O                                        4-Cl        H           n-Bu          O                                        4-CF.sub.3  H           (CH.sub.2).sub.3 Cl                                                                          O                                        4-Cl        H           (CH.sub.2).sub.3 Cl                                                                          O                                        4-Br        H           CH.sub.2 CF.sub.3                                                                            O                                        4-OCF.sub.3 H           CH.sub.2 CF.sub.3                                                                            O                                        4-SCF.sub.2 H                                                                              H           CH.sub.2 OMe  O                                        4-CF.sub.3  H           CH.sub.2 OEt  O                                        4-Cl        H           CH.sub.2 CO.sub.2 Me                                                                         O                                        4-Br        H           CH.sub.2 CO.sub.2 Me                                                                         O                                        4-OCF.sub.2 H                                                                              H           CH.sub.2 CN   O                                        4-OCF.sub.2 CF.sub.2 H                                                                     H           (CH.sub.2).sub.2 CN                                                                          O                                        4-CF.sub.3  H           (CH.sub.2).sub.2 CN                                                                          O                                        4-CF.sub.3  H           (CH.sub.2).sub.3 CN                                                                          O                                        4-CF.sub.3  H           CO.sub.2 Me   O                                        4-Cl        H           CO.sub.2 Me   O                                        4-Br        H           CO.sub.2 Me   O                                        4-F         H           CO.sub.2 Me   O                                        4-CF.sub.2 Cl                                                                              H           CO.sub. 2 Me  O                                        4-OCF.sub.3 H           CO.sub.2 Me   O                                        3,4-CF.sub.2 CF.sub.2 O                                                                    H           CO.sub.2 Me   O                                        3,4-OCF.sub.2 CF.sub.2 O                                                                   H           CO.sub.2 Me   O                                        3,4-(Me).sub.2 CCH.sub.2 O                                                                 H           CO.sub.2 Me   O                                        4-CF.sub.3  H           CO.sub.2 Et   O                                        4-Br        H           CO.sub.2 Et   O                                        4-Cl        H           CO.sub.2 Et   O                                        4-CF.sub.3  H           CO.sub.2 H    O                                        4-CF.sub.3  H           CO.sub.2 Na   O                                        4-CF.sub.3  H           CO.sub.2 Ph   O                                        4-F         H           CO.sub.2 PH   O                                        4-CF.sub.3  H           CO.sub.2 CH.sub.2 CCl.sub.3                                                                  O                                        4-CF.sub.3  H           CO.sub.2 CH.sub.2 CF.sub.3                                                                   O                                        4-CF.sub.3  H           CO.sub.2 (CH.sub.2)Cl                                                                        0                                        4-CF.sub.3  H           CO.sub.2 (CH.sub.2).sub.2 Br                                                                 O                                        4-CF.sub.3  H           CO.sub.2 CH.sub.2 CN                                                                         O                                        4-CF.sub.3  H           CO.sub.2 allyl                                                                               O                                        4-CF.sub.3  H           CO.sub.2 CH.sub.2 Ph                                                                         O                                        4-CF.sub.3  H           CO.sub.2 CH.sub.2 SMe                                                                        O                                        4-CF.sub.3  H           C(O)NH.sub.2  O                                        4-Cl        H           C(O)NH.sub.2  O                                        4-Br        H           C(O)NHMe      O                                        4-OCF.sub.3 H           C(O)NHMe      O                                        4-CF.sub.3  H           C(O)NMe.sub.2 O                                        4-Cl        H           C(O)NMe.sub.2 O                                        4-Br        H           C(O)NHEt      O                                        4-CF.sub.3  H           C(O)NHMe      O                                        4-CF.sub.3  H           C(O)NHallyl   O                                        4-CF.sub.3  H           C(O)N(Me)allyl                                                                               O                                        4-CF.sub.3  H           C(O)NHPh-4-Cl O                                        4-OCF.sub.3 H           C(S)NH.sub.2  O                                        4-CF.sub.3  H           C(S)NHMe      O                                        4-Cl        H           C(S)NMe.sub.2 O                                        4-Br        H           C(S)Me        O                                        4-OCF.sub.3 H           C(S)Et        O                                        4-CF.sub.3  H           C(S)NMe.sub.2 O                                        4-Cl        H           C(S)NHMe      O                                        4-Br        5-Cl        H             O                                        4-CF.sub.3  5-Cl        Me            O                                        4-OCF.sub.3 5-Cl        Et            O                                        4-Cl        5-Cl        H             O                                        4-SMe       5-Cl        H             O                                        4-CO.sub.2 Et                                                                              5-Cl        H             O                                        4-Br        5-Cl        CO.sub.2 Me   O                                        3-SMe       5-Cl        CO.sub.2 Me   O                                        4-CO.sub.2 Et                                                                              5-Cl        CO.sub.2 Me   O                                        4-CF.sub.2  5-Cl        Co.sub.2 Me   O                                        4-CF.sub.3  5-Cl        H             O                                        4-CF.sub.3  H           CO.sub.2 Me   O                                        4-OCF.sub.2 H                                                                              5-Cl        CO.sub.2 Me   O                                        4-Cl        5-Cl        CO.sub.2 Me   O                                        4-Br        5-Cl        C(O)Me        O                                        4-CF.sub.3  5-Cl        C(O)Et        O                                        4-OCF.sub.3 5-Cl        C(O)NMe.sub.2 O                                        4-CF.sub.3  5-F         H             O                                        4-Cl        5-F         H             O                                        4-Br        5-F         H             O                                        4-OCF.sub.2 H                                                                              5-F         H             O                                        4-Cl        5-F         CO.sub.2 Me   O                                        4-Br        5-F         CO.sub.2 Me   O                                        4-CF.sub.3  5-F         CO.sub.2 Me   O                                        4-OCF.sub.2 H                                                                              5-F         CO.sub.2 Me   O                                        4-Cl        5-F         CO.sub.2 Me   O                                        4-Br        5-OCF.sub. 2 H                                                                             CO.sub.2 Me   O                                        4-Cl        5-OCF.sub.2 H                                                                              CO.sub.2 Me   O                                        4-Br        5-OCF.sub.2 H                                                                              CO.sub.2 Me   O                                        4-CF.sub.3  5-OCF.sub.2 H                                                                              CO.sub.2 Me   O                                        4-OCF.sub.3 5-OCF.sub.2 H                                                                              CO.sub.2 Me   O                                        4-OCF.sub.2 H                                                                              5-OCF.sub.2 H                                                                              CO.sub.2 Me   O                                        4-Cl        5-Br        CO.sub.2 Me   O                                        4-Br        5-NO.sub.2  CO.sub.2 Me   O                                        4-CF.sub.3  5-CF.sub.3  CO.sub.2 Me   O                                        4-OCF.sub.3 5-OCH.sub.3 CO.sub.2 Me   O                                        4-CF.sub.3  5-OCH.sub.2 Ph                                                                             Me            O                                        4-CF.sub.3  5-C(O)Me    Et            O                                        4-CF.sub.3  5-OCF.sub.2 CF.sub.2 H                                                                     CO.sub.2 Me   O                                        4-CF.sub.3  5-I         Me            O                                        4-CF.sub.3  5-OCF.sub.3 Et            O                                        4-CF.sub.3  5-Et        C(O)Me        O                                        4-CF.sub.3  5-Me        C(O)CF.sub.3  O                                        4-CF.sub.3  5-CN        Me            O                                        4-CF.sub.3  5-OMe       CO.sub.2 Me   O                                        4-CF.sub.3  5-OMe       CO.sub.2 Et   O                                        4-CF.sub.3  5-OMe       H             O                                        4-Cl        5-OMe       H             O                                        4-CF.sub.3  5-CO.sub.2 Me                                                                              n-C.sub.6 H.sub.13                                                                           O                                        4-CF.sub.3  5-SCF.sub.2 H                                                                              C(O)H         O                                        4-CF.sub.3  5-SO.sub.2 Me                                                                              (CH.sub.2).sub.4 Cl                                                                          O                                        4-CF.sub.3  5,6-di-Cl   H             O                                        4-CF.sub.3  5,6-di-Cl   CO.sub.2 Me   O                                        4-CF.sub.3  4-F         H             O                                        4-Cl        4-F         CO.sub. 2 Me  O                                        4-Br        4-F         CO.sub.2 Me   O                                        4-CF.sub.3  4-Cl        H             O                                        4-OCF.sub.2 H                                                                              4-Cl        H             O                                        4-OCF.sub.2 H                                                                              4-Cl        CO.sub.2 Me   O                                        4-CF.sub.3  4-Br        H             O                                        4-CF.sub.3  4-Br        CO.sub.2 Me   O                                        4-CF.sub.3  6-Cl        CO.sub.2 Me   O                                        4-CF.sub.3  6-F         CO.sub.2 Me   O                                        4-CF.sub.3  6-CF.sub.3  CO.sub.2 Me   O                                        4-CF.sub.3  4-Cl        CO.sub.2 Me   O                                        4-CF.sub.3  4-F         CO.sub.2 Me   O                                        4-CF.sub.3  6-Br        CO.sub.2 Me   O                                        4-CF.sub.3  6-NO.sub.2  CO.sub.2 Me   O                                        4-CF.sub.3  6-Me        CO.sub.2 Me   O                                        4-CF.sub.3  4-Cl        CO.sub.2 Me   O                                        4-CF.sub.3  4-F         CO.sub.2 Me   O                                        4-CF.sub.3  4-Br        CO.sub.2 Me   O                                        4-Cl        H           H             S                                        4-CF.sub.3  H           Me            S                                        4-Cl        H           CO.sub.2 Me   S                                        4-CF.sub.3  H           H             S                                        4-Cl        H           Me            S                                        4-CF.sub.3  H           CO.sub.2 Me   S                                        4-Cl        5-Cl        H             S                                        4-Cl        5-F         Me            S                                        4-CF.sub.3  5-F         CO.sub.2 Me   S                                        4-CF.sub.3  H           Ph            O                                        4-OCF.sub.3 H           Ph            O                                        4-Cl        H           Ph            O                                        4-Br        H           Ph            O                                        4-CF.sub.3  H           4-F-Ph        O                                        4-OCF.sub.3 H           4-F-Ph        O                                        4-Cl        H           4-F-Ph        O                                        4-Br        H           4-F-Ph        O                                        4-CF.sub.3  5-F         Ph            O                                        4-OCF.sub.3 5-F         Ph            O                                        4-Cl        5-F         Ph            O                                        4-Br        5-F         Ph            O                                        4-CF.sub.3  5-F         4-Cl-Ph       O                                        4-OCF.sub.3 5-F         4-Cl-Ph       O                                        4-Cl        5-F         4-Cl-Ph       O                                        4-Br        5-F         4-Cl-Ph       O                                        4-CF.sub.3  5-F         4-F-Ph        O                                        4-OCF.sub.3 5-F         4-F-Ph        O                                        4-Cl        5-F         4-F-Ph        O                                        4-Br        5-F         4-F-Ph        O                                        4-CF.sub.3  5-F         Ph            O                                        4-OCF.sub.3 5-Cl        Ph            O                                        4-Cl        5-Cl        Ph            O                                        4-Br        5-Cl        Ph            O                                        4-CF.sub.3  5-Cl        4-F-Ph        O                                        4-OCF.sub.3 5-Cl        4-F-Ph        O                                        4-Cl        5-Cl        4-F-Ph        O                                        4-Br        5-Cl        4-F-Ph        O                                        4-CF.sub.3  5-Cl        4-Cl-Ph       O                                        4-OCF.sub.3 5-Cl        4-Cl-Ph       O                                        4-Cl        5-Cl        4-Cl-Ph       O                                        4-Br        5-Cl        4-Cl-Ph       O                                        4-CF.sub.3  5-Br        4-F-Ph        O                                        4-OCF.sub.3 5-Br        4-F-Ph        O                                        4-Cl        5-Br        4-F-Ph        O                                        4-Br        5-Br        4-F-Ph        O                                        4-CF.sub.3  5-Br        4-Cl-Ph       O                                        4-OCF.sub.3 5-Br        4-Cl-Ph       O                                        4-Cl        5-Br        4-Cl-Ph       O                                        4-Br        5-Br        4-F-Ph        O                                        ______________________________________                                    

                  TABLE 14                                                         ______________________________________                                         R.sub.1  R.sub.2   B          X    A                                           ______________________________________                                         4-CF.sub.2 Cl                                                                           H         H          O    O                                           4-CF.sub.3                                                                              H         H          O    O                                           4-Br     H         H          O    O                                           3-CF.sub.3                                                                              H         H          O    O                                           4-Cl     H         H          O    O                                           3-Cl     H         H          O    O                                           4-CF.sub.3                                                                              5-Br      H          O    O                                           4-Cl     5-Br      H          O    O                                           4-Br     5-Br      H          O    O                                           4-Cl     7-Br      H          O    O                                           4-CF.sub.3                                                                              7-Br      H          O    O                                           4-Br     7-Br      H          O    O                                           4-Cl     5-F       H          O    O                                           4-CF.sub.3                                                                              H         Me         O    O                                           4-OCF.sub.2 H                                                                           5-F       Me         O    O                                           4-Br     H         Me         O    O                                           4-OCF.sub.3                                                                             H         CO.sub.2 Me                                                                               O    O                                           4-CO.sub.2 Me                                                                           5-Cl      CO.sub.2 Me                                                                               O    O                                           4-Cl     H         CO.sub.2 CH.sub.2 CF.sub.3                                                                O    O                                           4-Cl     5-Cl      C(O)Me     O    O                                           4-CF.sub.3                                                                              5-OCF.sub.2 H                                                                            Me         O    O                                           4-CF.sub.3                                                                              5-F       CONHPh     O    O                                           4-Cl     5-Cl      n-Pr       O    O                                           4-CF.sub.3                                                                              5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               O    O                                           4-Cl     H         4-Cl-Ph    O    O                                           4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               S    O                                           4-CF.sub.2 Cl                                                                           H         H          O    S                                           4-Cl     5-F       H          O    S                                           4-CF.sub.3                                                                              H         H          O    S                                           4-Cl     H         H          O    S                                           4-Br     H         H          O    S                                           3-CF.sub.3                                                                              H         H          O    S                                           4-Cl     H         H          O    S                                           3-CF.sub.3                                                                              5-Cl      H          O    S                                           4-Cl     5-Cl      H          O    S                                           3-Cl     5-Cl      H          O    S                                           4-Br     5-Cl      H          O    S                                           4-Cl     5-Cl      H          O    S                                           4-CF.sub.3                                                                              6-Cl      H          O    S                                           3-CF.sub.3                                                                              6-Cl      H          O    S                                           4-Cl     6-Cl      H          O    S                                           3-Cl     6-Cl      H          O    S                                           4-Br     6-Cl      H          O    S                                           4-Cl     6-Cl      H          O    S                                           4-CF.sub.3                                                                              5-Br      H          O    S                                           3-CF.sub.3                                                                              5-Br      H          O    S                                           4-Cl     5-Br      H          O    S                                           3-Cl     5-Br      H          O    S                                           4-Br     5-Br      H          O    S                                           4-Cl     5-Br      H          O    S                                           4-CF.sub.3                                                                              4-Cl      H          O    S                                           4-Cl     4-Cl      H          O    S                                           4-Br     4-Cl      H          O    S                                           4-CF.sub.3                                                                              H         Me         O    S                                           4-OCF.sub.2 H                                                                           5-F       Me         O    S                                           4-Br     H         Me         O    S                                           4-OCF.sub.3                                                                             H         CO.sub.2 Me                                                                               O    S                                           4-CO.sub.2 Me                                                                           5-Cl      CO.sub.2 Me                                                                               O    S                                           4-Cl     H         CO.sub.2 CH.sub.2 CF.sub.3                                                                O    S                                           4-CF.sub.3                                                                              5-OCF.sub.2 H                                                                            Me         O    S                                           4-CF.sub.3                                                                              5-F       CONHPh     O    S                                           4-Cl     5-Cl      n-Pr       O    S                                           4-CF.sub.3                                                                              5-OCF.sub.2 H                                                                            CO.sub.2 Me                                                                               O    S                                           4-Cl     H         4-Cl-Ph    O    S                                           4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               S    S                                           4-CF.sub.2 Cl                                                                           H         H          O    NMe                                         4-Cl     5-F       H          O    NMe                                         4-CF.sub.3                                                                              H         Me         O    NMe                                         4-OCF.sub.2 H                                                                           5-F       Me         O    NMe                                         4-Br     H         Me         O    NMe                                         4-OCF.sub.3                                                                             H         CO.sub.2 Me                                                                               O    NMe                                         4-CO.sub.2 Me                                                                           5-Cl      CO.sub.2 Me                                                                               O    NMe                                         4-Cl     H         CO.sub.2 CH.sub.2 CF.sub.3                                                                O    NMe                                         4-CF.sub.3                                                                              5-OCF.sub.2 H                                                                            Me         O    NMe                                         4-CF.sub.3                                                                              5-F       CONHPh     O    NMe                                         4-Cl     5-Cl      n-Pr       O    NMe                                         4-Cl     H         4-Cl-Ph    O    NMe                                         4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               S    NMe                                         4-CF.sub.3                                                                              H         H          O    SO.sub.2                                    4-Cl     H         H          O    SO.sub.2                                    4-Br     H         H          O    SO.sub.2                                    3-CF.sub.3                                                                              H         H          O    SO.sub.2                                    4-Cl     H         H          O    SO.sub.2                                    3-Cl     H         H          O    SO.sub.2                                    4-CF.sub.3                                                                              5-Cl      H          O    SO.sub.2                                    3-CF.sub.3                                                                              5-Cl      H          O    SO.sub.2                                    4-Cl     5-Cl      H          O    SO.sub.2                                    3-Cl     5-Cl      H          O    SO.sub.2                                    4-Cl     5-Cl      H          O    SO.sub.2                                    4-CF.sub.3                                                                              6-Cl      H          O    SO.sub.2                                    3-CF.sub.3                                                                              6-Cl      H          O    SO.sub.2                                    4-Cl     6-Cl      H          O    SO.sub.2                                    3-Cl     6-Cl      H          O    SO.sub. 2                                   4-Br     6-Cl      H          O    SO.sub.2                                    4-Cl     6-Cl      H          O    SO.sub.2                                    4-Cl     5-Cl      Me         O    SO.sub.2                                    4-OCF.sub.3                                                                             H         Et         O    SO.sub.2                                    4-Cl     H         CO.sub.2 Me                                                                               O    SO.sub.2                                    4-OCF.sub.3                                                                             5-Cl      CO.sub.2 Et                                                                               O    SO.sub.2                                    3-CF.sub.3                                                                              H         H          O    SO(α).sup.1                           4-CF.sub.3                                                                              H         H          O    SO(α)                                 4-Br     H         H          O    SO(β).sup.1                            4-Cl     H         H          O    SO(α)                                 4-Cl     H         H          O    SO(β)                                  4-Cl     H         H          O    SO(α)                                 4-Cl     H         H          O    SO(β)                                  3-Cl     H         H          O    SO(α)                                 3-Cl     H         H          O    SO(β)                                  4-CF.sub.3                                                                              5-Cl      H          O    SO(α)                                 4-CF.sub.3                                                                              5-Cl      H          O    SO(β)                                  3-CF.sub.3                                                                              5-Cl      H          O    SO(α)                                 3-CF.sub.3                                                                              5-Cl      H          O    SO(β)                                  4-Cl     5-Cl      H          O    SO(α)                                 4-Cl     5-Cl      H          O    SO(β)                                  3-Cl     5-Cl      H          O    SO(α)                                 3-Cl     5-Cl      H          O    SO(β)                                  4-Br     5-Cl      H          O    SO(α)                                 4-Br     5-Cl      H          O    SO(β)                                  4-Cl     5-Cl      H          O    SO(α)                                 4-Cl     5-Cl      H          O    SO(β)                                  4-CF.sub.3                                                                              6-Cl      H          O    SO(α)                                 4-CF.sub.3                                                                              6-Cl      H          O    SO(β)                                  3-CF.sub.3                                                                              6-Cl      H          O    SO(α)                                 3-CF.sub.3                                                                              6-Cl      H          O    SO(β)                                  4-Cl     6-Cl      H          O    SO(α)                                 4-Cl     6-Cl      H          O    SO(β)                                  3-Cl     6-Cl      H          O    SO(α)                                 3-Cl     6-Cl      H          O    SO(β)                                  4-Br     6-Cl      H          O    SO(α)                                 4-Br     6-Cl      H          O    SO(β)                                  4-Cl     6-Cl      H          O    SO(α)                                 4-Cl     6-Cl      H          O    SO(β)                                  3-CF.sub.3                                                                              H         H          O    SO(β)                                  4-CF.sub.3                                                                              H         H          O    SO(β)                                  4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    N-allyl                                     4-OCF.sub.3                                                                             5-Cl      CO.sub.2 Me                                                                               O    N--CH.sub.2 Ph                              4-CF.sub.3                                                                              H         H          O    NH                                          4-CF.sub.3                                                                              H         CO.sub.2 Me                                                                               O    NH                                          4-CF.sub.3                                                                              5-Cl      H          O    NMe                                         4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    NMe                                         4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    NC(O)CH.sub.3                               4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    NCO.sub.2 CH.sub.3                          4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    NSO.sub.2 CH.sub.3                          4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    NCH.sub.2 Ph                                4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    N-allyl                                     4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    NCO.sub.2 C(CH.sub.3).sub.3                 4-CF.sub.3                                                                              H         Ph         O    S                                           4-OCF.sub.3                                                                             H         Ph         O    S                                           4-Cl     H         Ph         O    S                                           4-Br     H         Ph         O    S                                           4-CF.sub.3                                                                              H         4-F-Ph     O    S                                           4-OCF.sub.3                                                                             H         4-F-Ph     O    S                                           4-Cl     H         4-F-Ph     O    S                                           4-Br     H         4-F-Ph     O    S                                           4-CF.sub.3                                                                              5-F       Ph         O    S                                           4-OCF.sub.3                                                                             5-F       Ph         O    S                                           4-Cl     5-F       Ph         O    S                                           4-Br     5-F       Ph         O    S                                           4-CF.sub.3                                                                              5-F       4-Cl-Ph    O    S                                           4-Cl     5-F       4-Cl-Ph    O    S                                           4-Br     5-F       4-Cl-Ph    O    S                                           4-CF.sub.3                                                                              5-F       4-F-Ph     O    S                                           4-OCF.sub.3                                                                             5-F       4-F-Ph     O    S                                           4-Cl     5-F       4-F-Ph     O    S                                           4-Br     5-F       4-F-Ph     O    S                                           4-CF.sub.3                                                                              5-Cl      Ph         O    S                                           4-OCF.sub.3                                                                             5-Cl      Ph         O    S                                           4-Cl     5-Cl      Ph         O    S                                           4-Br     5-Cl      Ph         O    S                                           4-CF.sub.3                                                                              5-Cl      4-F-Ph     O    S                                           4-OCF.sub.3                                                                             5-Cl      4-F-Ph     O    S                                           4-Cl     5-Cl      4-F-Ph     O    S                                           4-Br     5-Cl      4-F-Ph     O    S                                           4-CF.sub.3                                                                              5-Cl      4-Cl-Ph    O    S                                           4-OCF.sub.3                                                                             5-Cl      4-Cl-Ph    O    S                                           4-Cl     5-Cl      4-Cl-Ph    O    S                                           4-CF.sub.3                                                                              5-Br      4-F-PH     O    S                                           4-OCF.sub.3                                                                             5-Br      4-F-Ph     O    S                                           4-Cl     5-Br      4-F-Ph     O    S                                           4-Br     5-Br      4-F-Ph     O    S                                           4-OCF.sub.3                                                                             5-Br      4-Cl-Ph    O    S                                           4-Cl     5-Br      4-Cl-Ph    O    S                                           4-Br     5-Br      4-Cl-Ph    O    S                                           4-CF.sub.3                                                                              5-Br      4-Cl-Ph    O    S                                           4-CF.sub.3                                                                              H         Ph         O    O                                           4-OCF.sub.3                                                                             H         Ph         O    O                                           4-Cl     H         Ph         O    O                                           4-Br     H         Ph         O    O                                           4-CF.sub.3                                                                              H         4-F-Ph     O    O                                           4-OCF.sub.3                                                                             H         4-F-Ph     O    O                                           4-Cl     H         4-F-Ph     O    O                                           4-Br     H         4-F-Ph     O    O                                           4-CF.sub.3                                                                              5-F       Ph         O    O                                           4-OCF.sub.3                                                                             5-F       Ph         O    O                                           4-Cl     5-F       Ph         O    O                                           4-Br     5-F       Ph         O    O                                           4-CF.sub.3                                                                              5-F       4-Cl-Ph    O    O                                           4-OCF.sub.3                                                                             5-F       4-Cl-Ph    O    O                                           4-Cl     5-F       4-Cl-Ph    O    O                                           4-Br     5-F       4-Cl-Ph    O    O                                           4-CF.sub.3                                                                              5-F       4-F-Ph     O    O                                           4-OCF.sub.3                                                                             5-F       4-F-Ph     O    O                                           4-Cl     5-F       4-F-Ph     O    O                                           4-Br     5-F       4-F-Ph     O    O                                           4-CF.sub.3                                                                              5-Cl      Ph         O    O                                           4-OCF.sub.3                                                                             5-Cl      Ph         O    O                                           4-Cl     5-Cl      Ph         O    O                                           4-Br     5-Cl      Ph         O    O                                           4-CF.sub.3                                                                              5-Cl      4-F-Ph     O    O                                           4-OCF.sub.3                                                                             5-Cl      4-F-Ph     O    O                                           4-Cl     5-Cl      4-F-Ph     O    O                                           4-Br     5-Cl      4-F-Ph     O    O                                           4-CF.sub.3                                                                              5-Cl      4-Cl-Ph    O    O                                           4-OCF.sub.3                                                                             5-Cl      4-Cl-Ph    O    O                                           4-Cl     5-Cl      4-Cl-Ph    O    O                                           4-Br     5-F       4-F-Ph     O    O                                           4-CF.sub.3                                                                              5-Br      4-F-PH     O    O                                           4-OCF.sub.3                                                                             5-Br      4-F-Ph     O    O                                           4-Cl     5-Br      4-F-Ph     O    O                                           4-Br     5-Br      4-F-Ph     O    O                                           4-CF.sub.3                                                                              5-Br      4-F-Ph     O    O                                           4-OCF.sub.3                                                                             5-Br      4-Cl-Ph    O    O                                           4-Cl     5-Br      4-Cl-Ph    O    O                                           4-Br     5-Br      4-Cl-Ph    O    O                                           4-CF.sub.3                                                                              5-Br      4-Cl-Ph    O    O                                           4-CF.sub.3                                                                              5-F       4-Cl-Ph    O    SO.sub.2                                    4-Cl     5-F       4-Cl-Ph    O    SO.sub.2                                    4-Br     5-F       4-Cl-Ph    O    SO.sub.2                                    4-CF.sub.3                                                                              5-Cl      4-Cl-Ph    O    SO.sub.2                                    4-OCF.sub.3                                                                             5-Cl      4-Cl-Ph    O    SO.sub.2                                    4-Cl     5-Cl      4-Cl-Ph    O    SO.sub.2                                    4-Br     5-Cl      4-Cl-Ph    O    SO.sub.2                                    4-CF.sub.3                                                                              H         4-Cl-Ph    O    SO.sub.2                                    4-OCF.sub.3                                                                             H         4-Cl-Ph    O    SO.sub.2                                    4-Cl     H         4-Cl-Ph    O    SO.sub.2                                    4-Br     H         4-Cl-Ph    O    SO.sub.2                                    4-CF.sub.3                                                                              5-F       4-Cl-Ph    O    SO                                          4-OCF.sub.3                                                                             5-F       4-Cl-Ph    O    SO                                          4-Cl     5-F       4-Cl-Ph    O    SO                                          4-Br     5-F       4-Cl-Ph    O    SO                                          4-CF.sub.3                                                                              5-Cl      4-Cl-Ph    O    SO                                          4-OCF.sub.3                                                                             5-Cl      4-Cl-Ph    O    SO                                          4-Cl     5-Cl      4-Cl-Ph    O    SO                                          4-Br     5-Cl      4-Cl-Ph    O    SO                                          4-CF.sub.3                                                                              H         4-Cl-Ph    O    SO                                          4-OCF.sub.3                                                                             H         4-Cl-Ph    O    SO                                          4-Cl     H         4-Cl-Ph    O    SO                                          4-Br     H         4-Cl-Ph    O    SO                                          4-CF.sub.3                                                                              5-F       4-Cl-Ph    O    NMe                                         4-OCF.sub.3                                                                             5-F       4-Cl-Ph    O    NMe                                         4-Cl     5-F       4-Cl-Ph    O    NMe                                         4-Br     5-F       4-Cl-Ph    O    NMe                                         4-CF.sub.3                                                                              5-Cl      4-Cl-Ph    O    NMe                                         4-OCF.sub.3                                                                             5-Cl      4-Cl-Ph    O    NMe                                         4-Cl     5-Cl      4-Cl-Ph    O    NMe                                         4-Br     5-Cl      4-Cl-Ph    O    NMe                                         4-CF.sub.3                                                                              H         4-Cl-Ph    O    NMe                                         4-OCF.sub.3                                                                             H         4-Cl-Ph    O    NMe                                         4-Cl     H         4-Cl-Ph    O    NMe                                         4-Br     H         4-Cl-Ph    O    NMe                                         4-CF.sub.3                                                                              5-Cl      4-Cl-Ph    O    O                                           4-OCF.sub.3                                                                             5-Cl      4-Cl-Ph    O    O                                           4-Cl     5-Cl      4-Cl-Ph    O    O                                           4-Br     5-Cl      4-Cl-Ph    O    O                                           4-OCF.sub.2 CF.sub.2 H                                                                  H         Ph         O    O                                           4-I      H         CH.sub.3   O    O                                           4-COCH.sub.3                                                                            H         CH.sub.3   O    O                                           4-OCF.sub.2 CF.sub.2 H                                                                  H         CH.sub.3   O    O                                           4-CF.sub.3                                                                              H         CO.sub.2 CH.sub.3                                                                         O    O                                           4-CF.sub.3                                                                              5-F       H          O    O                                           4-Br     5-F       H          O    O                                           4-OCF.sub.3                                                                             5-F       H          O    O                                           4-CF.sub.3                                                                              5-Cl      H          O    O                                           4-Br     5-Cl      H          O    O                                           4-OCF.sub.3                                                                             5-Cl      H          O    O                                           4-CF.sub.3                                                                              5-F       Me         O    O                                           4-Br     5-F       Me         O    O                                           4-OCF.sub.3                                                                             5-F       Me         O    O                                           4-CF.sub.3                                                                              H         CO.sub.2 Me                                                                               O    O                                           4-OCF.sub.3                                                                             H         CO.sub.2 Me                                                                               O    O                                           4-Cl     H         CO.sub.2 Me                                                                               O    O                                           4-Br     H         CO.sub.2 Me                                                                               O    O                                           4-CF.sub.3                                                                              5-F       CO.sub.2 Me                                                                               O    O                                           4-OCF.sub.3                                                                             5-F       CO.sub.2 Me                                                                               O    O                                           4-Cl     5-F       CO.sub.2 Me                                                                               O    O                                           4-Br     5-F       CO.sub.2 Me                                                                               O    O                                           4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    O                                           4-OCF.sub.3                                                                             5-Cl      CO.sub. 2 Me                                                                              O    O                                           4-Cl     5-Cl      CO.sub.2 Me                                                                               O    O                                           4-Br     5-Cl      CO.sub.2 Me                                                                               O    O                                           4-CF.sub.3                                                                              5-Br      CO.sub.2 Me                                                                               O    O                                           4-OCF.sub.3                                                                             5-Br      CO.sub.2 Me                                                                               O    O                                           4-Cl     5-Br      CO.sub.2 Me                                                                               O    O                                           4-Br     5-Br      CO.sub.2 Me                                                                               O    O                                           4-CF.sub.3                                                                              5-F       CO.sub.2 Me                                                                               O    S                                           4-OCF.sub.3                                                                             5-F       CO.sub.2 Me                                                                               O    S                                           4-Cl     5-F       CO.sub.2 Me                                                                               O    S                                           4-Br     5-F       CO.sub.2 Me                                                                               O    S                                           4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    S                                           4-OCF.sub.3                                                                             5-Cl      CO.sub.2 Me                                                                               O    S                                           4-Cl     5-Cl      CO.sub.2 Me                                                                               O    S                                           4-Br     5-Cl      CO.sub.2 Me                                                                               O    S                                           4-CF.sub.3                                                                              5-F       CO.sub.2 Me                                                                               O    N--CH.sub.3                                 4-OCF.sub.3                                                                             5-F       CO.sub.2 Me                                                                               O    N--CH.sub.3                                 4-Cl     5-F       CO.sub.2 Me                                                                               O    N--CH.sub.3                                 4-Br     5-F       CO.sub.2 Me                                                                               O    N--CH.sub.3                                 4-CF.sub.3                                                                              5-Cl      CO.sub.2 Me                                                                               O    N--CH.sub.3                                 4-OCF.sub.3                                                                             5-Cl      CO.sub.2 Me                                                                               O    N--CH.sub.3                                 4-Cl     5-Cl      CO.sub.2 Me                                                                               O    N--CH.sub.3                                 4-Br     5-Cl      CO.sub.2 Me                                                                               O    N--CH.sub.3                                 ______________________________________                                          .sup.1 α denotes cis relationship to substituent B; β denotes       trans relationship to substitutent B.                                    

                                      TABLE 15                                     __________________________________________________________________________     R.sub.1                                                                              R.sub.2                                                                              B        Y             A                                           __________________________________________________________________________     4-OCF.sub.3                                                                          H     H        Me            CH.sub.2                                    4-CF.sub.3                                                                           H     H        C(O)Me        CH.sub.2                                    4-F   H     CO.sub.2 Me                                                                             Me            CH.sub.2                                    4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                             C(O)Me        CH.sub.2                                    4-CF.sub.3                                                                           H     Me       C(O)CF.sub.3  CH.sub.2                                    4-Cl  H     Me       CO.sub.2 Et   CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 CH.sub.2 CF.sub.3                                                              Me            CH.sub.2                                    4-OCF.sub.2 H                                                                        H     CO.sub.2 Et                                                                             Me            CH.sub.2                                    4-OCF.sub.3                                                                          H     CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                           Me            CH.sub.2                                    4-Br  H     CONHMe   Me            CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             C(O)Me        CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             Me            CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             CO.sub.2 Me   CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             C(O)Me        CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             Me            CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             CO.sub.2 Me   CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             C(O)Me        CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             C(O)Me        CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             CO.sub.2 Me   CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             CO.sub.2 Me   CH.sub.2                                    4-CF.sub.3                                                                           H     H        CO.sub.2 -t-Bu                                                                               CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(iPr)P(O)(OCH.sub.3)(CH.sub.3)                                                             CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SP(O)(OC.sub.2 H.sub.5).sub.2                                                                CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(iPr).sub.2 CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(iPr)P(O)(OC.sub.2 H.sub.5)(Ph)                                                            CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SP(O)(OiPr).sub.2                                                                            CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(sec Bu).sub.2                                                                             CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR34##    CH.sub.2                                    4-Cl  H     CO.sub.2 Me                                                                              ##STR35##    CH.sub.2                                    4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                              ##STR36##    CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR37##    CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR38##    CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR39##    CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  4-Cl Phenyl                                                                              ##STR40##    CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR41##    CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR42##    CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR43##    CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR44##    CH.sub.2                                    4-Cl  H     CO.sub.2 Me                                                                              ##STR45##    CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR46##    CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR47##    CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR48##    CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                              ##STR49##    CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR50##    CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR51##    CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR52##    CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-Cl  H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-F   H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 Ph                                                                           CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      CH.sub. 2                                   4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR53##    CH.sub.2                                    4-Cl  H     CO.sub.2 Me                                                                              ##STR54##    CH.sub.2                                    4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                              ##STR55##    CH.sub.2                                    4-OCF.sub.2                                                                          H     CO.sub.2 Me                                                                              ##STR56##    CH.sub.2                                    4-F   H     CO.sub.2 Me                                                                              ##STR57##    CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR58##    CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub. 2 Me                                                                             ##STR59##    CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR60##    CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                              ##STR61##    CH.sub.2                                    4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR62##    CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR63##    CH.sub.2                                    4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR64##    CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             Me            CH.sub.2                                    4-OCF.sub.3                                                                          5-Cl  CO.sub.2 Me                                                                             Me            CH.sub.2                                    4-Br  5-Cl  CO.sub.2 Me                                                                             Me            CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             COCH.sub.3    CH.sub.2                                    4-OCF.sub.3                                                                          5-F   CO.sub.2 Me                                                                             COCH.sub.3    CH.sub.2                                    4-Br  5-F   CO.sub.2 Me                                                                             COCH.sub.3    CH.sub.2                                    4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             CO.sub.2 CH.sub.3                                                                            CH.sub.2                                    4-OCF.sub.3                                                                          5-Cl  CO.sub.2 Me                                                                             CO.sub. 2 CH.sub.3                                                                           CH.sub.2                                    4-Br  5-Cl  CO.sub.2 Me                                                                             CO.sub.2 CH.sub.3                                                                            CH.sub.2                                    4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             COCF.sub.3    CH.sub.2                                    4-OCF.sub.3                                                                          5-F   CO.sub.2 Me                                                                             COCF.sub.3    CH.sub.2                                    4-Br  5-F   CO.sub.2 Me                                                                             COCF.sub.3    CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-ClPh   Me            CH.sub.2                                    4-OCF.sub.3                                                                          4-Cl  4-ClPh   Me            CH.sub.2                                    4-Br  4-Cl  4-ClPh   Me            CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-ClPh   COCH.sub.3    CH.sub.2                                    4-OCF.sub.3                                                                          4-CL  4-ClPh   COCH.sub.3    CH.sub.2                                    4-Br  4-Cl  4-ClPh   COCH.sub.3    CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-ClPh   CO.sub.2 CH.sub.3                                                                            CH.sub.2                                    4-OCF.sub.3                                                                          4-Cl  4-ClPh   CO.sub.2 CH.sub.3                                                                            CH.sub.2                                    4-Br  4-Cl  4-ClPh   CO.sub.2 CH.sub.3                                                                            CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-ClPh   COCF.sub.3    CH.sub.2                                    4-OCF.sub.3                                                                          4-Cl  4-ClPh   COCF.sub.3    CH.sub.2                                    4-Br  4-Cl  4-ClPh   COCF.sub.3    CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   CH.sub.2                                    4-OCF.sub.3                                                                          4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   CH.sub.2                                    4-Br  4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-ClPh   Me            CH.sub.2                                    4-OCF.sub.3                                                                          4-Cl  4-FPh    Me            CH.sub.2                                    4-Br  4-Cl  4-FPh    Me            CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-FPh    COCH.sub.3    CH.sub.2                                    4-OCF.sub.3                                                                          4-Cl  4-FPh    COCH.sub.3    CH.sub.2                                    4-Br  4-Cl  4-FPh    COCH.sub.3    CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            CH.sub.2                                    4-OCF.sub.3                                                                          4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            CH.sub.2                                    4-Br  4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            CH.sub.2                                    4-CF.sub.3                                                                           4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          CH.sub.2                                    4-OCF.sub.3                                                                          4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          CH.sub.2                                    4-Br  4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          CH.sub.2                                    4-CF.sub.3                                                                           H     Me       Me            NMe                                         4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             Me            S                                           4-CF.sub.3                                                                           5-Cl  Me       Me            NMe                                         4-CF.sub.3                                                                           5-Cl  Me       C(O)Me        S                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             C(O)Me        NMe                                         4-CF.sub.3                                                                           5-F   Me       C(O)Me        SO                                          4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SCCl.sub.3    O                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SCCl.sub.3    NMe                                         4-CF.sub.3                                                                           H     Me       CO.sub.2 Me   O                                           4-CF.sub.3                                                                           5-OCF.sub.2 H                                                                        CO.sub.2 Me                                                                             n-Pr          NMe                                         4-CF.sub.3                                                                           5-CF.sub.3                                                                           Me       C(O)CF.sub.3  O                                           4-CF.sub.3                                                                           5-CF.sub.3                                                                           Me       C(O)CF.sub.3  NMe                                         4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SMe           O                                           4-CF.sub.3                                                                           H     H        Me            S                                           4-CF.sub.3                                                                           H     H        CO.sub.2 Me   S                                           4-CF.sub.3                                                                           H     H        C(O)Me        S                                           4-CF.sub.3                                                                           5-Cl  H        C(O)Me        S                                           4-CF.sub.3                                                                           5-Cl  H        CO.sub.2 Me   S                                           4-CF.sub.3                                                                           5-Cl  H        Me            S                                           4-Cl  H     H        C(O)Me        S                                           4-Cl  H     H        Me            S                                           4-Cl  5-Cl  H        C(O)Me        S                                           4-Cl  5-Cl  H        Me            S                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR65##    O                                           4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR66##    O                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR67##    O                                           4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                              ##STR68##    O                                           4-CF.sub.3                                                                           4-F   4-Cl-Phenyl                                                                              ##STR69##    O                                           4-CF.sub.3                                                                           5-F   4-Cl-Phenyl                                                                              ##STR70##    O                                           4-CF.sub.3                                                                           H     4-Cl-Phenyl                                                                              ##STR71##    O                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR72##    O                                           4-Cl  H     CO.sub.2 Me                                                                              ##STR73##    O                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR74##    O                                           4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR75##    O                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR76##    O                                           4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                              ##STR77##    O                                           4-CF.sub.3                                                                           4-F   4-Cl-Phenyl                                                                              ##STR78##    O                                           4-CF.sub.3                                                                           5-F   4-Cl-Phenyl                                                                              ##STR79##    O                                           4-CF.sub.3                                                                           H     4-Cl-Phenyl                                                                              ##STR80##    O                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-Cl  H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-OCF.sub.3                                                                          H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-CF.sub.3                                                                           4-F   4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-CF.sub.3                                                                           5-F   4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-CF.sub.3                                                                           H     4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     O                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-Cl  H     CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-OCF.sub.3                                                                          H     CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-F   H     CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-CF.sub.3                                                                           4-F   4-Cl-Phenyl                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-CF.sub.3                                                                           5-F   4-Cl-Phenyl                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-CF.sub.3                                                                           H     4-Cl-Phenyl                                                                             SN(CH.sub.3)SO.sub.2 Ph                                                                      O                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR81##    O                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR82##    O                                           4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR83##    O                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR84##    O                                           4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                              ##STR85##    O                                           4-CF.sub.3                                                                           4-F   4-Cl-Phenyl                                                                              ##STR86##    O                                           4-CF.sub.3                                                                           5-F   4-Cl-Phenyl                                                                              ##STR87##    O                                           4-CF.sub.3                                                                           H     4-Cl-Phenyl                                                                              ##STR88##    O                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR89##    S                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR90##    S                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(iPr).sub.2 S                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR91##    S                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR92##    S                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(s-Bu).sub.2                                                                               S                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR93##    S                                           4-Cl  H     CO.sub.2 Me                                                                              ##STR94##    S                                           4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                              ##STR95##    S                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR96##    O                                           4-Cl  H     CO.sub.2 Me                                                                              ##STR97##    O                                           4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                              ##STR98##    O                                           4-OCF.sub.3                                                                          H     CO.sub.2 Me                                                                              ##STR99##    O                                           4-F   H     CO.sub.2 Me                                                                              ##STR100##   O                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR101##   O                                           4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR102##   O                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR103##   O                                           4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                              ##STR104##   O                                           4-CF.sub.3                                                                           4-F   4-Cl-Phenyl                                                                              ##STR105##   O                                           4-CF.sub.3                                                                           5-F   4-Cl-Phenyl                                                                              ##STR106##   O                                           4-CF.sub.3                                                                           H     4-Cl-Phenyl                                                                              ##STR107##   O                                           4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                              ##STR108##   S                                           4-Cl  H     CO.sub.2 Me                                                                              ##STR109##   S                                           4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                              ##STR110##   S                                           4-OCF.sub.3                                                                          H     CO.sub.2 Me                                                                              ##STR111##   S                                           4-F   H     CO.sub.2 Me                                                                              ##STR112##   S                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR113##   S                                           4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR114##   S                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR115##   S                                           4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                              ##STR116##   S                                           4-CF.sub.3                                                                           4-F   4-Cl-Phenyl                                                                              ##STR117##   S                                           4-CF.sub.3                                                                           5-F   4-Cl-Phenyl                                                                              ##STR118##   S                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     S                                           4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     S                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     S                                           4-CF.sub.3                                                                           5-Cl  4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     S                                           4-CF.sub.3                                                                           4-F   4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     S                                           4-CF.sub.3                                                                           5-F   4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     S                                           4-CF.sub.3                                                                           H     4-Cl-Phenyl                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     S                                           4-Cl  H     CO.sub.2 Me                                                                              ##STR119##   NCH.sub. 3                                  4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                              ##STR120##   NCH.sub.3                                   4-OCF.sub.3                                                                          H     CO.sub.2 Me                                                                              ##STR121##   NCH.sub.3                                   4-F   H     CO.sub.2 Me                                                                              ##STR122##   NCH.sub.3                                   4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                              ##STR123##   NCH.sub.3                                   4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                              ##STR124##   NCH.sub.3                                   4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                              ##STR125##   NCH.sub.3                                   4-CF.sub.3                                                                           5-Cl  4-ClPhenyl                                                                               ##STR126##   NCH.sub.3                                   4-CF.sub.3                                                                           4-F   4-ClPhenyl                                                                               ##STR127##   NCH.sub.3                                   4-CF.sub.3                                                                           5-F   4-ClPhenyl                                                                               ##STR128##   NCH.sub.3                                   4-CF.sub.3                                                                           H     4-ClPhenyl                                                                               ##STR129##   NCH.sub.3                                   4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-Cl  H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-OCF.sub.3                                                                          H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-F   H     CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-CF.sub.3                                                                           5-Cl  4-ClPhenyl                                                                              SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-CF.sub.3                                                                           4-F   4-ClPhenyl                                                                              SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-CF.sub.3                                                                           5-F   4-ClPhenyl                                                                              SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-CF.sub.3                                                                           H     4-ClPhenyl                                                                              SN(iPr)SO.sub.2 CH.sub.3                                                                     NCH.sub.3                                   4-CF.sub.3                                                                           H     CO.sub.2 Me                                                                             SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-Cl  H     CO.sub.2 Me                                                                             SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-OCF.sub.2 H                                                                        H     CO.sub.2 Me                                                                             SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-OCF.sub. 3                                                                         H     CO.sub.2 Me                                                                             SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-F   H     CO.sub.2 Me                                                                             SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-CF.sub.3                                                                           4-F   CO.sub.2 Me                                                                             SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-CF.sub.3                                                                           5-Cl  4-ClPhenyl                                                                              SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-CF.sub.3                                                                           4-F   4-ClPhenyl                                                                              SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-CF.sub.3                                                                           5-F   4-ClPhenyl                                                                              SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-CF.sub.3                                                                           H     4-ClPhenyl                                                                              SN(s-Bu)SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                  NCH.sub.3                                   4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             Me            S                                           4-OCF.sub.3                                                                          5-Cl  CO.sub.2 Me                                                                             Me            S                                           4-Br  5-Cl  CO.sub.2 Me                                                                             Me            S                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             COCH.sub.3    S                                           4-OCF.sub.3                                                                          5-F   CO.sub.2 Me                                                                             COCH.sub.3    S                                           4-Br  5-F   CO.sub.2 Me                                                                             COCH.sub.3    S                                           4-CF.sub.3                                                                           4-Cl  CO.sub.2 Me                                                                             CO.sub.2 CH.sub.3                                                                            S                                           4-OCF.sub.3                                                                          5-Cl  CO.sub.2 Me                                                                             CO.sub.2 CH.sub.3                                                                            S                                           4-Br  5-Cl  CO.sub.2 Me                                                                             CO.sub.2 CH.sub.3                                                                            S                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             COCF.sub.3    S                                           4-OCF.sub.3                                                                          5-F   CO.sub.2 Me                                                                             COCF.sub.3    S                                           4-Br  5-F   CO.sub.2 Me                                                                             COCF.sub.3    S                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   Me            S                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   Me            S                                           4-Br  4-Cl  4-ClPh   Me            S                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   COCH.sub.3    S                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   COCH.sub.3    S                                           4-Br  4-Cl  4-ClPh   COCH.sub.3    S                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   CO.sub.2 CH.sub.3                                                                            S                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   CO.sub.2 CH.sub.3                                                                            S                                           4-Br  4-Cl  4-ClPh   CO.sub.2 CH.sub.3                                                                            S                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   COCF.sub.3    S                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   COCF.sub.3    S                                           4-Br  4-Cl  4-ClPh   COCF.sub.3    S                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   S                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   S                                           4-Br  4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   S                                           4-CF.sub.3                                                                           4-Cl  4-FPh    Me            S                                           4-OCF.sub.3                                                                          4-Cl  4-FPh    Me            S                                           4-Br  4-Cl  4-FPh    Me            S                                           4-CF.sub.3                                                                           4-Cl  4-FPh    COCH.sub.3    S                                           4-OCF.sub.3                                                                          4-Cl  4-FPh    COCH.sub.3    S                                           4-Br  4-Cl  4-FPh    COCH.sub.3    S                                           4-CF.sub.3                                                                           4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            S                                           4-OCF.sub.3                                                                          4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            S                                           4-Br  4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            S                                           4-CF.sub.3                                                                           4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          S                                           4-OCF.sub.3                                                                          4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          S                                           4-Br  4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          S                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             Me            O                                           4-OCF.sub.3                                                                          5-Cl  CO.sub.2 Me                                                                             Me            O                                           4-Br  5-Cl  CO.sub.2 Me                                                                             Me            O                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             COCH.sub.3    O                                           4-OCF.sub.3                                                                          5-F   CO.sub.2 Me                                                                             COCH.sub.3    O                                           4-Br  5-F   CO.sub.2 Me                                                                             COCH.sub.3    O                                           4-CF.sub.3                                                                           5-Cl  CO.sub.2 Me                                                                             CO.sub.2 CH.sub.3                                                                            O                                           4-OCF.sub.3                                                                          5-Cl  CO.sub.2 Me                                                                             CO.sub.2 CH.sub.3                                                                            O                                           4-Br  5-Cl  CO.sub.2 Me                                                                             CO.sub.2 CH.sub.3                                                                            O                                           4-CF.sub.3                                                                           5-F   CO.sub.2 Me                                                                             COCF.sub.3    O                                           4-OCF.sub.3                                                                          5-F   CO.sub.2 Me                                                                             COCF.sub.3    O                                           4-Br  5-F   CO.sub.2 Me                                                                             COCF.sub.3    O                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   Me            O                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   Me            O                                           4-Br  4-Cl  4-ClPh   Me            O                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   COCH.sub.3    O                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   COCH.sub.3    O                                           4-Br  4-Cl  4-ClPh   COCH.sub.3    O                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   CO2CH.sub.3   O                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   CO2CH.sub.3   O                                           4-Br  4-Cl  4-ClPh   CO2CH.sub.3   O                                           4-CF.sub.3                                                                           4-Cl  4-ClPh   COCF.sub.3    O                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   COCF.sub.3    O                                           4-Br  4-Cl  4-ClPh   COCF.sub.3    O                                           4-CH.sub.3                                                                           4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   O                                           4-OCF.sub.3                                                                          4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   O                                           4-Br  4-Cl  4-ClPh   CO.sub.2 CH.sub.2 CH.sub.3                                                                   O                                           4-CF.sub.3                                                                           4-Cl  4-FPh    Me            O                                           4-OCF.sub.3                                                                          4-Cl  4-FPh    Me            O                                           4-Br  4-Cl  4-FPh    Me            O                                           4-CF.sub.3                                                                           4-Cl  4-FPh    COCH.sub.3    O                                           4-OCF.sub.3                                                                          4-Cl  4-FPh    COCH.sub.3    O                                           4-Br  4-Cl  4-FPh    COCH.sub.3    O                                           4-CF.sub.3                                                                           4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            O                                           4-OCF.sub.3                                                                          4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            O                                           4-Br  4-Cl  4-FPh    CO.sub.2 CH.sub.3                                                                            O                                           4-CF.sub.3                                                                           4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          O                                           4-OCF.sub.3                                                                          4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          O                                           4-Br  4-Cl  4-FPh    COCH.sub.2 CH.sub.3                                                                          O                                           __________________________________________________________________________

                  TABLE 16                                                         ______________________________________                                         R.sub.1 R.sub.2 B         A       R.sub.a.sup.1                                                                       R.sub.a.sup.2                           ______________________________________                                         4-CF.sub.3                                                                             5-Cl    H         CHMe    H    H                                       4-OCF.sub.3                                                                            5-Cl    H         CHMe    H    H                                       4-Cl    5-Cl    H         CHMe    H    H                                       4-Br    5-Cl    H         CHMe    H    H                                       4-OCF.sub.2 H                                                                          5-Cl    H         CHMe    H    H                                       4-CF.sub.3                                                                             5-F     H         CHMe    H    H                                       4-OCF.sub.3                                                                            5-F     H         CHMe    H    H                                       4-Cl    5-F     H         CHMe    H    H                                       4-Br    5-F     H         CHMe    H    H                                       4-OCF.sub.2 H                                                                          5-F     H         CHMe    H    H                                       4-CF.sub.3                                                                             5-Cl    H         CH(i-Pr)                                                                               H    H                                       4-Cl    5-Cl    H         CH(i-Pr)                                                                               H    H                                       CF.sub.3                                                                               5-Cl    Me        CHMe    H    H                                       OCF.sub.3                                                                              5-Cl    Me        CH(i-Pr)                                                                               H    H                                       OCF.sub.2 H                                                                            5-Cl    Me        C(Me).sub.2                                                                            H    H                                       Cl      5-Cl    Me        C(Me).sub.2                                                                            H    H                                       CF.sub.3                                                                               5-Cl    CO.sub.2 Me                                                                              C(Me).sub.2                                                                            H    H                                       OCF.sub.3                                                                              5-Cl    CO.sub.2 Me                                                                              C(Me).sub.2                                                                            H    H                                       OCF.sub.2 H                                                                            5-Cl    CO.sub.2 Me                                                                              CHEt    H    H                                       Cl      5-Cl    CO.sub.2 Me                                                                              CHEt    H    H                                       CF.sub.3                                                                               5-F     Ph        CHMe    H    H                                       OCF.sub.3                                                                              5-F     Ph        CHMe    H    H                                       OCF.sub.2 H                                                                            5-F     Ph        CHMe    H    H                                       Cl      5-F     Ph        CHMe    H    H                                       CF.sub.3                                                                               5-F     CO.sub.2 Me                                                                              CHMe    H    H                                       OCF.sub.3                                                                              5-F     CO.sub.2 Me                                                                              CHMe    H    H                                       CF.sub.3                                                                               H       H         CH.sub.2                                                                               Me   H                                       OCF.sub.3                                                                              H       H         CH.sub.2                                                                               Me   H                                       CF.sub.3                                                                               H       4-F--Ph   CH.sub.2                                                                               Me   H                                       OCF.sub.3                                                                              H       4-F--Ph   CH.sub.2                                                                               Me   H                                       CF.sub.3                                                                               5-Cl    CO.sub.2 Me                                                                              CH.sub.2                                                                               Me   H                                       OCF.sub.3                                                                              5-Cl    CO.sub.2 Me                                                                              CH.sub.2                                                                               Me   H                                       CF.sub.3                                                                               5-F     CO.sub.2 Me                                                                              CH.sub.2                                                                               Me   H                                       OCF.sub.3                                                                              5-F     CO.sub.2 Me                                                                              CH.sub.2                                                                               Me   H                                       CF.sub.3                                                                               5-Cl    Me        CH.sub.2                                                                               Me   Me                                      OCF.sub.3                                                                              5-Cl    Me        CH.sub.2                                                                               Me   Me                                      CF.sub.3                                                                               5-F     Ph        CH.sub.2                                                                               Me   Me                                      OCF.sub.3                                                                              5-F     Ph        CH.sub.2                                                                               Me   Me                                      CF.sub.3                                                                               5-Cl    CO.sub.2 Me                                                                              CH.sub.2                                                                               Me   Me                                      OCF.sub.3                                                                              5-Cl    CO.sub.2 Me                                                                              CH.sub.2                                                                               Me   Me                                      CF.sub.3                                                                               H       H         O       Me   H                                       OCF.sub.3                                                                              H       H         O       Me   H                                       CF.sub.3                                                                               H       H         O       Me   Me                                      OCF.sub.3                                                                              H       H         O       Me   Me                                      CF.sub.3                                                                               5-Cl    CO.sub.2 Me                                                                              O       Me   H                                       OCF.sub.3                                                                              5-Cl    CO.sub.2 Me                                                                              O       Me   H                                       CF.sub.3                                                                               5-Cl    CO.sub.2 Me                                                                              O       Me   H                                       OCF.sub.3                                                                              5-Cl    CO.sub.2 Me                                                                              O       Me   H                                       CF.sub.3                                                                               5-F     CO.sub.2 Me                                                                              O       Me   H                                       OCF.sub.3                                                                              5-F     CO.sub.2 Me                                                                              O       Me   H                                       CF.sub.3                                                                               5-F     Ph        O       Me   H                                       OCF.sub.3                                                                              5-F     Ph        O       Me   H                                       CF.sub.3                                                                               5-F     Me        O       Me   H                                       OCF.sub.3                                                                              5-F     Me        O       Me   H                                       CF.sub.3                                                                               H       H         S       Me   H                                       OCF.sub.3                                                                              H       H         S       Me   H                                       CF.sub.3                                                                               H       Ph        S       Me   H                                       OCF.sub.3                                                                              5-Cl    Ph        S       Me   H                                       CF.sub.3                                                                               5-Cl    H         S       Me   Me                                      OCF.sub.3                                                                              5-Cl    H         S       Me   Me                                      CF.sub.3                                                                               5-F     Me        S       Me   H                                       OCF.sub.3                                                                              5-F     Me        S       Me   H                                       OCF.sub.3                                                                              5-Cl    H         CH.sub.2                                                                               Me   H                                       OCF.sub.3                                                                              5-Cl    H         CH.sub.2                                                                               Me   H                                       CF.sub.3                                                                               5-Cl    H         CH.sub.2                                                                               Me   Me                                      OCF.sub.3                                                                              5-Cl    H         CH.sub.2                                                                               Me   Me                                      CF.sub.3                                                                               5-F     H         CH.sub.2                                                                               Me   Me                                      OCF.sub.3                                                                              5-F     H         CH.sub.2                                                                               Me   Me                                      ______________________________________                                    

FORMULATION AND USE

The compounds of this invention will generally be used in formulation with a carrier comprising a liquid or solid diluent or an organic solvent. Useful formulations of the compounds of Formula I can be prepared in conventional ways. They include dusts, granules, pellets, solutions, suspensions, emulsions, wettable powders, emulsifiable concentrates, dry flowables and the like. Many of these can be applied directly. Sprayable formulations can be extended in suitable media and used at spray volumes of from about one to several hundred liters per hectare. High strength compositions are primarily used as intermediates for further formulation. The formulations, broadly, contain about 1% to 99% by weight of active ingredient(s) and at least one of a) about 0.1% to 20% surfactant(s) and b) about 5% to 99% solid or liquid diluent(s). More specifically, they will contain these ingredients in the following approximate proportions:

    ______________________________________                                                     Active  Percent by Weight                                                      Ingredient                                                                             Diluent(s)                                                                               Surfactant(s)                                    ______________________________________                                         Wettable Powders                                                                             25-90     0-74      1-10                                         Oil Suspensions,                                                                             1-50      40-95     0-35                                         Emulsions, Solutions,                                                          (including Emulsifiable                                                        Concentrates)                                                                  Dusts         1-25      70-99     0-5                                          Granules and Pellets                                                                         1-95      5-99      0-15                                         High Strength 90-99     0-10      0-2                                          Compositions                                                                   ______________________________________                                    

Lower or higher levels of active ingredient can, of course, be present depending on the intended use and the physical properties of the compound. Higher ratios of surfactant to active ingredient are sometimes desirable, and are achieved by incorporation into the formulation or by tank mixing.

Typical solid diluents are described in Watkins, et al., "Handbook of Insecticide Dust Diluents and Carriers", 2nd Ed., Dorland Bookds, Caldwell, N.J. The more absorptive diluents are preferred for wettable powders and the denser ones for dusts. Typical liquid diluents and solvents are described in Marsden, "Solvents Guide," 2nd Ed., Interscience, New York, 1950. Solubility under 0.1% is preferred for suspension concentrates; solution concentrates are preferably stable against phase separation at 0° C. "McCutcheon's Detergents and Emulsifiers Annual", Allured Publ. Corp., Ridgewood, N.J., as well as Sisely and Wood, "Encyclopedia of Surface Active Agents", Chemical Publ. Co., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foam, caking, corrosion, microbiological growth, etc. Preferably, ingredients should be approved by the U.S. environmental Protection Agency for the use intended.

The methods of making such compositions are well known. Solutions are prepared by simply mixing the ingredients. Fine solid compositions are made by blending and, usually, grinding as in a hammer or fluid energy mill. Suspensions are prepared by wet milling (see, for example, U.S. Pat. No. 3,060,084). Granules and pellets can be made by spraying the active material upon preformed granular carriers or by agglomeration techniques. See Browning, "Agglomeration", Chemical Engineering, Dec. 4, 1967, pages 147 and following, and "Perry's Chemical Engineer's Handbook", 4th Ed., McGraw-Hill, New York, 1963, pages 8 to 59 and following.

Many of the compounds of the invention are most efficacious when applied in the form of an emulsifiable concentrate mixed with a spray oil or spray oil concentrate. Although any oil can be used as a spray oil, spray oils usually have these characteristics: they are not phytotoxic to the crop sprayed, and they have appropriate viscosity. Petroleum based oils are commonly used for spraying. In some areas, crop oils are preferred such as they following:

    ______________________________________                                         Common Crop Oils Used as Spray Oils                                            ______________________________________                                         Corn Oil            Linseed Oil                                                Cottonseed Oil      Soybean Oil                                                Coconut Oil         Sunflower Oil                                              Rapeseed Oil        Olive Oil                                                  Peanut Oil          Palm Oil                                                   Safflower Oil       Sesame Oil                                                 Mustardseed Oil     Caster Oil                                                 ______________________________________                                    

The following oils also meet the criteria for a spray oil: mineral, fish and cod liver oil.

Spray oil concentrates comprise a spray oil together with one or more additional ingredients such as emulsifiers and wetting agents. A number of useful spray oil and spray oil concentrates can be found in "A Guide to Agricultural Spray Adjuvants Used in the United States" by Thomson, Thomson Publications, California, 1986.

Examples of useful formulations of compounds of the present invention are as follows:

EXAMPLE A

    ______________________________________                                         Emulsifiable Concentrate                                                       ______________________________________                                         methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoro-                                                          20%                                                  methyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1                                 c][1,4]benzoxazine-3a-carboxylate.                                             blend of oil soluble sulfonates                                                                          10%                                                  and polyoxyethylene ethers                                                     isophorone                70%                                                  ______________________________________                                    

The ingredients are combined and stirred with gentle warming to speed solution. A fine screen filter is included in packaging operation to insure the absence of any extraneous undissolved material in the product.

EXAMPLE B

    ______________________________________                                         Wettable Powder                                                                ______________________________________                                         methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoro-                                                          30%                                                  methyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1                                 c][1,4]benzoxazine-3a-carboxylate.                                             sodium alkylnaphthalenesulfonate                                                                          2%                                                  sodium ligninsulfonate     2%                                                  synthetic amorphous silica                                                                                3%                                                  kaolinite                 63%                                                  ______________________________________                                    

The active ingredient is mixed with the inert materials in a blender. After grinding in a hammermill, the material is re-blended and sifted through a 50 mesh screen.

    ______________________________________                                         Dust                                                                           ______________________________________                                         Wettable powder of Example B                                                                         10%                                                      pyrophyllite (powder) 90%                                                      ______________________________________                                    

The wettable powder and the pyrophyllite diluent are thoroughly blended and then packaged. The product is suitable for use as a dust.

EXAMPLE D

    ______________________________________                                         Granule                                                                        ______________________________________                                         methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoro-                                                          10%                                                  methyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1                                 c][1,4]benzoxazine-3a-carboxylate.                                             matter, 0.71/0.30 mm; U.S.S. No.                                                                         90%                                                  25-50 sieves)                                                                  ______________________________________                                    

The active ingredient is dissolved in a volatile solvent such as acetone and sprayed upon dedusted and pre-warmed attapulgite granules in a double cone blender. The acetone is then driven off by heating. The granules are then allowed to cool and are packaged.

EXAMPLE E

    ______________________________________                                         Granule                                                                        ______________________________________                                         Wettable powder of Example B                                                                         15%                                                      gypsum                69%                                                      potassium sulfate     16%                                                      ______________________________________                                    

The ingredients are blended in a rotating mixer and water sprayed on to accomplish granulation. When most of the material has reached the desired range of 0.1 to 0.42 mm (U.S. Ser. No. 18 to 40 sieves), the granules are removed, dried, and screened. Oversize material is crushed to produce additional material in the desired range. These granules contain 4.5% active ingredient.

EXAMPLE F

    ______________________________________                                         Solution                                                                       ______________________________________                                         methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoro-                                                             25%                                               methyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1-c][1,4]                         benzoxazine-3a-carboxylate   25%                                               N-methyl-pyrrolidone         75%                                               ______________________________________                                    

The ingredients are combined and stirred to produce a solution suitable for direct, low volume application.

EXAMPLE G

    ______________________________________                                         Aqueous Suspension                                                             ______________________________________                                         Methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoro-                                                            40%                                                methyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1-c][1,4]                         benzoxazine-3a-carboxylate.                                                    polyacrylic acid thickener  0.3%                                               dodecyclophenol polyethylene glycol                                                                        0.5%                                               ether                                                                          disodium phosphate          1.0%                                               monosodium phosphate        0.5%                                               polyvinyl alcohol           1.0%                                               water                       56.7%                                              ______________________________________                                    

The ingredients are blended and ground together in a sand mill to produce particles essentially all under 5 microns in size.

EXAMPLE H

    ______________________________________                                         Oil Suspension                                                                 ______________________________________                                         Methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoro-                                                            35.0%                                              methyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1-c][1,4]                         benzoxazine-3a-carboxylate.                                                    blend of polyalcohol carboxylic                                                                            6.0%                                               esters and oil soluble petroleum                                               sulfonates                                                                     xylene range solvent        59.0%                                              ______________________________________                                    

The ingredients are combined and ground together in a sand mill to produce particles essentially all below 5 microns. The product can be used directly, extended with oils, or emulsified in water.

    ______________________________________                                         Bait Granules                                                                  ______________________________________                                         Methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoro-                                                            3.0%                                               methyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1-c][1,4]                         benzoxazine-3a-carboxylate.                                                    blend of polyethoxylated nonyl-                                                                            9.0%                                               phenols and sodium dodecyl-                                                    benzene sulfonates                                                             ground up corn cobs         88.0%                                              ______________________________________                                    

The active ingredient and surfactant blend are dissolved in a suitable solvent such as acetone and sprayed onto the ground corn cobs. The granules are then dried and packaged.

Compound of Formula I can also be mixed with one or more other insecticides, fungicides, nematocides, bactericides, acaricides, or other biologically active compounds to form a multi-component pesticide giving an even broader spectrum of effective agricultural protection. Examples of other agricultural protectants with which compounds of the present invention can be mixed or formulated are:

INSECTICIDES

3-hydroxy-N-methylcrotonamide(dimethylphosphate)ester (monocrotophos)

methylcarbamic acid, ester with 2,3-dihydro-2,2-dimethyl-7-benzofuranol (carbofuran)

O-[2,4,5-trichloro-α-(chloromethyl)benzyl]phosphoric acid, O',O'-dimethyl ester (tetrachlorvinphos)

2-mercaptosuccinic acid, diethyl ester, S-ester with thionophosphoric acid, dimethyl ester (malathion)

phosphorothioic acid, O,O-dimethyl, O-p-nitrophenyl ester (methyl parathion)

methylcarbamic acid, ester with α-naphthol (carbaryl) methyl O-methylcarbamoyl)thiolacetohydroxamate (methomyl)

N'-(4-chloro-o-tolyl)-N,N-dimethylformamidine (chlordimeform)

O,O-diethyl-O-(2-isopropyl-4-methyl-6-pyrimidylphosphorothioate (diazinon)

octachlorocamphene (toxaphene)

O-ethyl O-p-nitrophenyl phenylphosphonothioate (EPN)

(S)-α-cyano-m-phenoxybenzyl(1R,3R)-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate (deltamethrin)

Methyl N',N'-dimethyl-N-[(methylcarbamoyl)oxy]-1-thiooxamimidate (oxamyl)

cyano(3-henoxyphenyl)-methyl-4-chloro-α-(1-methylethyl)benzeneacetate (fenvalerate)

(3-phenoxyphenyl)methyl(±)-cis,trans-3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropanecarboxylate (permethrin)

α-cyano-3-phenoxybenzyl 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane carboxylate (cypermethrin)

O-ethyl-S-(p-chlorophenyl)ethylphosphonodithioate (profenofos)

phosphorothiolothionic acid, O-ethyl-O-[4-(methylthio)phenyl]-S-n-propyl ester (sulprofos).

Additional insecticides are listed hereafter by their common names: triflumuron, diflubenzuron, methoprene, buprofezin, thiodicarb, acephate, azinphos-methyl, chlorpyrifos, dimethoate, fonophos, isofenos, methiadathion, methamidiphos, monocrotophos, phosmet, phosphamidon, phosalone, pirimicarb, phorate, profenofos, terbufos, trichlorfon, methoxychlor, bifenthrin, biphenate, cyfluthrin, fenpropathrin, fluvalinate, flucythrinate, tralomethrin, metaldehyde and rotenone.

FUNGICIDES

methyl 2-benzimidazolecarbamate (carbendazim)

tetramethylthiuram disulfide (thiuram)

n-dodecylguanidine acetate (dodine)

manganese ethylenebisdithiocarbamate (maneb)

1,4-dichloro-2,5-dimethoxybenzene (chloroneb)

methyl 1-(butylcarbamoyl)-2-benzimidazolecarbamate (benomyl)

1-[2-(2,4-dichlorophenyl)-4-propyl-1,3-dioxolan-2-ylmethyl]-1H-1,2,4-triazole (propiconazole)

2-cyano-N-ethylcarbamoyl-2-methoxyiminoacetamide (cymoxanil)

1-(4-chlorophenoxy)-3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl)-2-butanone (triadimefon)

N-(trichloromethylthio)tetrahydrophthalimide (captan)

N-(trichloromethylthio)phthalimide (folpet)

1-[[[bis(4-fluorophenyl)[]methyl]sily]methyl]-1H-1,2,4-triazole.

NEMATOCIDES

S-methyl 1-(dimethycarbamoyl)-N-(methylcarbamoyloxy)thioformimidate

S-methyl 1-carbamoyl-N-(methylcarbamoyloxy)thioformimidate

N-isopropylphosphoramidic acid, O-ethyl O'-[4-(methylthio)-m-tolyl]diester (fenamiphos).

BACKTERICIDES

tribasi copper sulfate

streptomycin sulfate.

ACARICIDES

senecionic acid, ester with 2-sec-butyl-4,6-dinitrophenol (binapacryl)

6-methyl-1,3-dithiolol[4,5-c]quinoxalin-2-one (oxythioquinox)

ethyl 4,4'-dichlorobenzilate (chlorobenzilate)

1,1-bis(p-chlorophenyl)-2,2,2-trichloroethanol (dicofol)

bis(pentachloro-2,4-cyclopentadien-1-yl) (dienochlor)

tricyclohexyltin hydroxide (cyhexatin)

trans-5-(4-chlorophenyl)-N-cyclohexyl-4-methyl-2-oxo-thiazolidine-3-carboxamide (hexythiazox)

amitraz

propargite

fenbutatin-oxide

bisclofentezin.

BIOLOGICAL

Bacillus thuringiensis

Avermectin B.

UTILITY

The compounds of this invention exhibit activity against a wide spectrum of foliar and soil inhabiting arthropods which are pests of growing and stored agronomic crops, forestry, greenhouse crops, ornamentals, nursery crops, stored food and fiber products, livestock, household, and public and animal health. Those skilled in the art will recognize that not all compounds are equally effective against all pests but the compounds of this invention display activity against:

larvae of the order Lepidoptera including fall and beet armyworm and other Spodoptera spp., tobacco budworm, corn earworm and other Heliothis spp., European corn borer, navel orangeworm, stalk/stem borers and other pyralids, cabbage and soybean loopers and other loopers, codling moth, graph berry moth and other tortricids, black cutworm, spotted cutworm, other cutworms and other noctuids, diamondback moth, green cloverworm, velvetbean caterpillar, green cloverworm, pink bollworm, gypsy moth, and spruce budworm;

foliar feeding larvae and adults of the order Coleoptera including Colorado potato beetle, Mexican bean beetle, flea beetle, Japanese beetles, and other leaf beetles, boll weevil, rice water weevil, granary weevil, rice weevil and other weevil pests, and soil inhabiting insects such as Western corn rootworm and other Diabrotica spp., Japanese beetle, European chafer and other coleopteran grubs, and wireworms;

adults and larvae of the orders Hemiptera and Hompotera including tarnished plant bug and other plant bugs (miridae), aster leafhopper and other leafhoppers (cicadellidae), rice planthopper, brown planthopper, and other planthoppers (fulgoroidea), psylids, whiteflies (aleurodidae), aphids (aphidae), scales (coccidae and diaspididae), lace bugs (tingidae), stink bugs (pentatomidae), cinch bugs and other seed buts (lygaeidae), cicadas (cicadidae), spittlebugs (cerocopids), squash bugs (coreidae), red bugs and cotton stainers (pyrrhocoridae);

adults, larvae and eggs of the order acari (mites) including European red mite, two spotted spider mite, rust mites, McDaniel mite, and foliar feed mites;

adults and immatures of the order Orthoptera including grasshoppers;

adults and immatures of the order Diptera including leafminers, midges, fruit flies (tephritidae), and soil maggots;

adults and immatures of the order Thysanoptera including onion thrips and other foliar feeding thrips;

insect pests of the order Hymenoptera including carpenter ants, bees, hornets and wasps;

insect pests of the order Diptera including house flies, stable flies, face flies, horn flies, blow flies, and other muscoid fly pests, horse flies, deer flies and other Brachycera, mosquitoes, black flies, biting midges, sand flies, sciarids, and other Nematocera;

insect pests of the order Orthoptera including cockroaches and crickets;

insect pests of the order Isoptera including the Easter subterranean termite and other termites;

insect pests of the order Mallphaga and Anoplura including the head louse, body louse, chicken head louse and other sucking and chewing parasitic lice that attack man and animals;

insect pest of the order Siphonoptera including the cat flea, dog flea and other fleas.

The specific species for which control is exemplified are: fall armyworm, Spodoptera fruigiperda; tobacco budworm, Heliothis virescens; boll weevil, Anthonomus grandis; aster leafhopper, Macrosteles fascifrons; sorther corn rootworm, Diabrotica undecimpunctata. The pest control protection afforded by these compounds of the present invention is limited, however, to these species.

APPLICATION

Arthropod pests are controlled and protection of agronomic crops, animal and human health is achieved by applying one or more of the Formula I compounds of this invention, in an effective amount, to the locus of infestation, to the area to be protected, or directly on the pests to be controlled. Because of the diversity of habitat and behavior of these arthropod pest species, many different methods of application are employed. A preferred method of application is by spraying with equipment that distributes the compound in the environment of the pests, on the foliage, animal, person, or premise, in the solid or animal, to the plant part that is infested or needs to be protected. Alternatively, granular formulations of these compounds can be applied to or incorporated into the soil. Other methods of application can also be employed including direct and residual sprays, aerial, baits, eartags, boluses, foggers, aerosols, and many others.

The compounds of this invention can be applied in their pure state, but most often application will be of a formulation comprising one or more compounds of this invention, with suitable carriers, diluents and surfactants depending on the contemplated end use. A preferred method of application involves spraying a water dispersion of refined oil solution of the compounds. Combinations with spray oils, spray oil concentrations, and synergists such as piperonyl butoxide often enhance the efficacy of the compounds of Formula I.

The rate of application of the Formula I compounds required for effective control will depend on such factors as the species of arthropod to be controlled, the pest's life cycle, life stage, its size, location, time of year, host crop or animal, feeding behavior, mating behavior, ambient moisture, temperature, etc. In general, application rates of about 0.01 to 2 kg of active ingredient per hectare are sufficient to provide large-scale effective control of pests in agronomic ecosystems under normal circumstances, but as little as 0.001 kg/hectare or as much as 8 kg/hectare may be required. For nonagronomic applications, effective use rates will range from about 0.1 t 5 mg/square foot but as little as 0.01 mg/square foot or as much as 15 mg/square foot may be required.

The following Examples demonstrate the control efficacy of the compounds of Formula I on specific insect pests wherein Compounds 1 through 44 are described in Table 17 and Compounds 45 and 46 in Table 18; and Compound 47 in Table 19.

                  TABLE 17                                                         ______________________________________                                          ##STR130##                                                                    CMPD  R.sub.1    R.sub.2                                                                               A    Y    B      m.p. °C.                       ______________________________________                                          1    4-CF.sub.3 H      O    H    H      157.5-158.5                            2    4-Cl       H      O    H    H      183-185                                3    4-Br       H      O    H    H      200-202                                4    4-CF.sub.3 H      O    H    Ph     183.5-185                              5    4-OCF.sub.2 CF.sub.2 H                                                                    H      O    H    Ph     190-191                                6    4-Cl       H      O    H    Ph     186-188                                7    4-CF.sub.3 H      O    H    Me     186-187                                8    4-I        H      O    H    Me       162-163.5                            9    4-COMe     H      O    H    Me     174- 177                              10    4-OCF.sub.2 CF.sub.2 H                                                                    H      O    H    Me     oil                                   11    4-CF.sub.3 H      O    H    Ph     106-116                               12    4-OCF.sub.3                                                                               5-Cl   O    H    Ph     140-146                               13    4-CF.sub.3 5-F    O    H    CO.sub.2 Me                                                                             177-181.5                           14    4-OCF.sub.3                                                                               5-F    O    H    4-ClPh 135-139                               15    4-Cl       5-F    O    H    4-ClPh 190-191                               16    4-CF.sub.3 5-F    O    H    4-ClPh 80-84                                 17    4-CF.sub.3 6-Cl   O    H    Ph       215-215.5                           18    4-Cl       6-Cl   O    H    Ph     180-181                               19    4-Br       6-Cl   O    H    Ph     173-175                               20    4-CF.sub.3 H      SO.sub.2                                                                            H    Me     265-266                               21    4-Cl       H      SO.sub.2                                                                            H    Me     192-194                               22    4-CF.sub.3 H      S    H    Ph     238-240                               23    4-CF.sub.3 H      S    H    Me     188-189                               24    4-Cl       H      S    H    Me     169-170                               25    4-Br       H      S    H    Me     163-165                               26    4-CF.sub.3 5-Cl   O    H    4-FPh  178-179                               27    4-CF.sub.3 5-Cl   O    Me   4-FPh  155-156                               28    4-OCF.sub.3                                                                               5-Cl   O    H    4-FPh  110-112                               29    4-Br       5-Cl   O    H    4-FPh  200-201                               30    4-CF.sub.3 5-F    O    H    Ph     176-178                               31    4-Br       5-F    O    H    Ph     162-163                               32    4-Cl       5-F    O    H    Ph     192-193                               33    4-OCF.sub.3                                                                               5-F    O    H    Ph     79-81                                 34    4-OCF.sub.3                                                                               5-Cl   O    H    H      157-158                               35    4-CF.sub.3 5-F    O    H    Me     171-172                               36    4-Br       5-F    O    H    Me     143-145                               37    4-OCF.sub.3                                                                               5-F    O    H    Me     124-126                               38    4-OCF.sub.3                                                                               5-F    O    H    H      138-139                               39    4-Cl       5-F    O    H    H      170-172                               40    4-CF.sub.3 5-F    O    Me   H      158-160                               41    4-CF.sub.3 5-Cl   O    H    H      171-172                               42    4-Br       5-Cl   O    H    H      177-179                               43    4-CF.sub.3 5-F    O    H    H      171-173                               44    4-Br       5-F    O    H    H      182-183                               ______________________________________                                    

                  TABLE 18                                                         ______________________________________                                          ##STR131##                                                                    CMPD     R.sub.1                                                                               R.sub.2   B   Y       m.p. °C.                          ______________________________________                                         45       CF.sub.3                                                                              H         H   H       219-221                                  46       CF.sub.3                                                                              Br        H   H       196-198                                  ______________________________________                                    

                  TABLE 19                                                         ______________________________________                                          ##STR132##                                                                    CMPD     R.sub.1                                                                               R.sub.2   B    Y     m.p. °C.                           ______________________________________                                         47       CF.sub.3                                                                              H         CH.sub.3                                                                            H     215-217                                   ______________________________________                                    

EXAMPLE 6 Fall Armyworm

Test units, each consisting of an 8-ounce plastic cup containing a layer of wheat germ diet, approximately 0.5 cm thick, were prepared. Ten third-instar larvae of fugal armyworm (Spodoptera frugiperda) were placed into each cup. Solutions of each of the test compounds (acetone/distilled water 75/25 solvent) were sprayed onto the cups, a single solution per set of three cups. Spraying was accomplished by passing the cups, on a conveyer belt, directly beneath a flat fan hydraulic nozzle which discharged the spray at a rate of 0.5 pounds of active ingredient per acre (about 0.55 kg/ha) at 30 p.s.i. The cups were then covered and held at 27° C. and 50% relative humidity for 72 hours, after which time readings were taken. The results are tabulated below.

    ______________________________________                                         Compound      % Mortality                                                      ______________________________________                                         11            100                                                              12            100                                                              13            100                                                              14            100                                                              15            100                                                              16            100                                                              26            100                                                              27            100                                                              28            100                                                              29            100                                                              30            100                                                              31            100                                                              32            100                                                              33            100                                                              ______________________________________                                    

EXAMPLE 7 Tobacco Budworm

The test procedure of Example 6 was repeated for efficacy against third-instar larvae of the tobacco budworm (Heliothis virescens) except that mortality was assessed at 48 hours. The results are tabulated below.

    ______________________________________                                         Compound      % Mortality                                                      ______________________________________                                         11            100                                                              12            100                                                              13             83                                                              14            100                                                              15            100                                                              16            100                                                              26            100                                                              27            100                                                              28            100                                                              29            100                                                              30            100                                                              31             40                                                              33            100                                                              ______________________________________                                    

EXAMPLE 8 Southern Corn Rootworm

Test units, each consisting of an 8-ounce plastic cup containing 1 sprouted corn seed, were prepared. Sets of three test units were sprayed as described in Example 6 with individual solutions of the test compounds. After the spray on the cups had dried, five third-instar larvae of the southern corn rootworm (Diabrotica undecimpunctata howardi) were placed into each cup. A moistened dental wick was inserted into each cup to prevent drying and the cups were then covered. The cups were then held at 27° C. and 50% relative humidity for 48 hours, after which time mortality readings were taken. Of the compounds tests on Southern rootworm, the following tabulations depicts the activity:

    ______________________________________                                         Compound      % Mortality                                                      ______________________________________                                         11            100                                                              12            100                                                              13            100                                                              14            100                                                              15            100                                                              16            100                                                              26            100                                                              27            100                                                              28            100                                                              29            100                                                              30            100                                                              31            100                                                              32            100                                                              33            100                                                              ______________________________________                                    

EXAMPLE 9 Boll Weevil

Five adult boll weevils (Anthonomus grandis) were placed into each of a series of 9-ounce cups. The test procedure employed was then otherwise the same as in Example 6. Mortality readings were taken 48 hours after treatment. Of the compounds tested on boll weevil, the following tabulation depicts the activity:

    ______________________________________                                         Compound      % Mortality                                                      ______________________________________                                         11            100                                                              12            100                                                              13             93                                                              15            100                                                              16             93                                                              30            100                                                              31            100                                                              32            100                                                              ______________________________________                                    

EXAMPLE 10 Aster Leafhopper

Test units were prepared from a series of 12-ounce cups, each containing oat (Avena Sativa) seedlings in a 1-inch layer of sterilized soil. The test units were sprayed as described in Example 6 with indiviudual solutions of the below-listed compounds. After the oats had dried from the spraying, between 10 and 15 adult aster leafhoppers (Mascrosteles fascifrons) were aspirated into each of the covered cups. The cups were held at 27° C. and 50% relative humidity for 48 hours, after which time mortality readings were taken. Of the compounds tested on aster leafhopper, the following tabulation depicts the activity:

    ______________________________________                                         Compound      % Mortality                                                      ______________________________________                                         11            88                                                               12            86                                                               13            100                                                              16            100                                                              26            87                                                               27            100                                                              28            95                                                               29            88                                                               30            100                                                              33            82                                                               ______________________________________                                     

What is claimed is:
 1. A compound of Formula I ##STR133## wherein: Q is ##STR134## G is O or S; A is a 0, 1 or 2-atom bridge comprising 0 to 2 carbon atoms, 0 to 1 oxygen atoms, 0 to 1 S(O)_(q) groups or 0 to 1 NR₆ groups wherein each carbon atom is optionally substituted with 1 to 2 substituents selected from R_(a) ; A being other than NR⁶ when Q is Q-8;B is H, C₁ to C₆ alkyl, C₃ to C₆ cycloalkyl optionally substituted with 1 to 2 halogens or 1 to 2 CH₃, C₄ to C₆ cycloalkylalkyl, C₁ to C₆ haloalkyl, C₂ to C₆ alkenyl, C₂ to C₆ alkynyl, C₂ l to C₆ alkoxyalkyl, C₂ to C₆ cyanoalkyl, C₃ to C₈ alkoxycarbonylalkyl, CO₂ R₃, C(O)R₃, C(O)NR₃ R₄, C(S)NR₃ R₄, C(S)R₃, C(S)SR₃, phenyl, phenyl substituted with (R₅)p, benzyl, benzyl substituted with 1 to 3 substituents independently selected from W, or OR₇ when Q is Q₁ to Q-5; W is halogen, CN, NO₂, C₁ to C₂ alkyl, C₁ to C₂ haloalkyl, C₁ to C₂ alkoxy, C₁ to C₂ haloalkoxy, C₁ to C₂ alkylthio, C₁ to C₂ haloalkylthio, C₁ to C₂ alkylsulfonyl or C₁ to C₂ haloalkylsulfonyl; R₁, R₂ and R₅ are independently selected from R₃, halogen, CN, N₃, SCN, NO₂, OR₃, SR₃, SOR₃, SO₂ R₃, OC(O)R₃, OSO₂ R₃, CO₂ R₃, C(O)R₃, C(O)NR₃ R₄, SO₂ NR₃ R₄, NR₃ R₄, NR₄ C(O)R₃, OC(O)NHR₃, NR_(r) C(O)NHR₃ and NR₄ SO₂ R₃, or when m, n or p is 2, R₁, R₂ or R₅ are --OCH₂ O--, --OCH₂ CH₂ O--, or --CH₂ Ch₂ O--, each of which are substituted with 1 to 4 halogen atoms or 1 to 2 methyl groups; R₃ is H, C₁ to C₆ alkyl, C₁ to C₆ haloalkyl, C₂ to C₆ alkenyl, C₂ to C₆ haloalkenyl, C₂ to C₆ alkynyl, C₂ to C₆ haloalkynyl, C₂ to C₆ alkoxyalkyl, C₂ to C₆ alkylthioalkyl, C₁ to C₆ nitroalkyl, C₂ to C₆ cyanoalkyl, C₃ to C₈ alkoxycarbonylalkyl, C₃ to C₆ cycloalkyl, C₃ to C₆ halocycloalkyl, phenyl, benzyl, or phenyl or benzyl substituted with 1 to 3 substituents independently selected from W; R₄ is H, C₁ to C₄ alkyl or R₃ and R₄ are taken together as (CH₂)₄, (CH₂)₅ or (CH₂ CH₂ OCH₂ CH₂); R₆ is H, C₁ to C₄ alkyl, C₁ to C₄ haloalkyl, C₂ to C₄ alkenyl, C₂ to C₄ haloalkenyl, C₂ to C₄ alkynyl, phenyl optionally substituted with W, or benzyl optionally substituted with W; R₇ is H, C₁ to C₄ alkyl, C₂ to C₄ alkenyl, C₂ to C₄ alkynyl, C₂ to C₄ alkylcarbonyl, C₂ to C₄ alkoxycarbonyl; R_(a) is independently selected from H, C₁ to C₆ alkyl, C₂ to C₄ alkoxycarbonyl and phenyl optionally substituted with 1 to 3 substituents independently selected from W; X is O or S; n is 1 to 2; m is 1 to 3; p is 1 to 3; q is 0 to 2; Y is H, C₁ to C₆ alkyl, C₂ to C₆ alkoxyalkyl, CHO, C₂ to C₆ alkylcarbonyl, C₂ to C₆ alkoxycarbonyl, C₂ to C₆ haloalkylcarbonyl, C₁ to C₆ alkylthio, C₁ to C₆ haloalkylthio, phenylthio, phenylthio substituted with 1 to 3 substituents independently selected from W, or S-J; J is ##STR135## R₈ and R₁₂ are independently selected from C₁ to C₆ alkyl, C₁ to C₆ haloalkyl, C₃ to C₆ cycloalkyl, C₄ to C₇ cycloalkylalkyl, phenyl optionally substituted with 1 to 2 substituents independently selected from W, benzyl optionally substituted with 1 to 2 substituents independently selected from W, phenethyl optionally substituted with 1 to 2 substituents independently selected from W, C₂ to C₆ cyanoalkyl, C₂ to C₆ alkoxyalkyl, C₃ to C₈ alkoxycarbonylalkyl and C₄ to C₈ dialkylaminocarbonylalkyl, or R₈ and R₁₂ are taken together as (CH₂)₄, (CH₂)₅ or (CH₂)₂ O(CH₂)₂ ; R₉ is F, C₁ to C₂₂ alkyl, C₁ to C₆ haloalkyl, C₁ to C₂₂ alkoxy, C₂ to C₈ dialkylamino, piperidinyl, pyrollidinyl, morpholino, C₁ to C₄ haloalkoxy, C₁ to C₄ alkoxy substituted with cyano, nitro, C₂ to C₄ alkoxy, C₄ to C₈ alkoxyalkoxy, C₁ to C₂ alkylthio, C₂ to C₃ alkoxycarbonyl, C₃ to C₅ dialkylaminocarbonyl or phenyl, or R₉ is phenyl optionally substituted with 1 to 2 substituents independently selected from W, or phenoxy optionally substituted with 1 to 2 substituents independently selected from W; R₁₀ and R₁₁ are independently selected from C₁ to C₄ alkyl, C₂ to C₄ haloalkyl and phenyl optionally substituted with 1 to 2 substituents independently selected from W, or R₁₀ and R₁₁ are taken together as (CH₂)₂, (CH₂)₃ or CH₂ C(CH₃)₂ CH₂ ; t is 0 to 2; and Y₁ is O or S.
 2. A compound according to claim 1 wherein:A is CR₁ R_(a), S, O or NR₆ ; B is H, C₁ to C₆ alkyl, C₁ to C₆ haloalkyl, C₂ to C₆ alkenyl, C₂ to C₆ alkynyl, C₂ to C₆ alkoxyalkyl, C₃ to C₈ alkoxycarbonylalkyl, CO₂ R₃, C(O)R₃, C(O)NR₃ R₄, C(S)NR₃ R₄, C(S)R₃, C(S)SR₃, phenyl or phenyl substituted by (R₅)p; W is Cl, F, Br, CN, CF₃, C₁ to C₂ alkyl, C₁ to C₂ alkoxy, OCF₂ H, OCF₃ or NO₂ ; R₂ is R₃, halogen, CN, SCN, NO₂, OR₃ or SR₃ ; R₃ is H, C₁ to C₄ alkyl, C₁ to C₂ haloalkyl, C₃ to C₄ alkenyl, C₃ to C₄ haloalkenyl, propargyl, phenyl, benzyl, or phenyl or benzyl substituted with one of F, Cl, Br, CF₃, OCF₃, OCF₂ H or NO₂ ; p is 1 or 2; m is 1 or 2; X is O; Y is H, C₁ to C₄ alkyl, SCH₃, SCCl₃, SO₂ CH₃, SC₆ H₅, 2--NO₂ --C₆ H₄ S, C(O)CH₃, C(O)CH₂ CH₃, C(O)CF₃ ; CO₂ CH₃, CO₂ CH₂ CH₃, or S-J; J is J₁, J₂, J₃, J₄ or J₅ ; R₈ and R₁₂ are independently selected from C₁ to C₆ alkyl, C₁ to C₆ haloalkyl, C₅ to C₆ cycloalkyl, C₃ to C₈ alkoxycarbonylalkyl, phenyl, benzyl and phenethyl, each phenyl, benzyl and phenethyl optionally substituted with W, or, R₈ and R₁₂ are taken together as (CH₂)₄, (CH₂)₅ or (CH₂)₂ O(CH₂)₂ ; R₁₀ and R₁₁ are independently selected from C₁ to C₃ alkyl or phenyl; and t is
 2. 3. A compound according to claim 2 wherein:B is H, C₁ to C₄ alkyl, C₃ to C₄ alkoxycarbonylalkyl, CO₂ R₃, C(O)R₃, phenyl or phenyl substituted with (R₅)p; R₁ is halogen, CN, SCN, NO₂, OR₃, SR₃, SO₂ R₃, CO₂ R₃, C(O)R₃ or is R₃ with one substituent in the 4-position; R₅ is H, R₃, halogen, CN, SCN, NO₂, OR₃, SR₃, SO₂ R₃, C(O)R₃, OSO₂ R₃, CO₂ R₃, C(O)R₃, C(O)NR₃ R₄, SO₂ NR₃ R₄ or NR₃ R₄ ; or, when m or p is 2; R₁ and R₅ are taken together as --CH₂ C(CH₃)₂ O--, OCH₂ CH₂ O--, OCF₂ CF₂ O-- or --CF₂ CF₂ O-- to form a 5- or 6-membered fused ring; R₃ is C₁ to C₄ alkyl, C₁ to C₂ haloalkyl, C₃ to C₄ alkenyl or propargyl; R₄ is H or CH₃ ; R_(a) is H, CH₃, CO₂ CH₃ or CO₂ CH₂ CH₃ ; m and p are independently 1 or 2 and one substituent is in the para-position; Y is H, CH₃, COCH₃, CO₂ CH₃ or S-J; J is J₁ or J₂ ; R₈ is C₁ to C₄ alkyl or phenyl optionally substituted with Cl or CH₃ ; R₉ is C₁ to C₂₀ alkyl, C₁ to C₂₀ alkoxy, C₁ to C₆ haloalkyl, dimethylamino, phenyl optionally substituted with Cl or CH₃, or, R₉ is C₁ to C₄ alkoxy substituted with C₂ to C₄ alkoxy or 1 to 6 halogens; and G is S.
 4. A compound according to claim 3 wherein:R₁ is Cl, F, Br, CF₃, CN, OCF₃, OCF₂ H, OCF₂ CF₂ H or SCF₂ H; R₂ and R₅ are independently H, CL, F, Br, CN, CF₃, CH₃, OCH(CH₃)₂, OCF₂ H, OCF₃, SCH₃, SCF₂ H, NO₂ or OCH₂ CF₃ ; B is H, CH₃, CH₂ CH₃, CH(CH₃)₂, CO₂ CH₃, CO₂ CH₂ CH₃, phenyl or phenyl substituted with (R₅)p; and R_(a) is H or CH₃.
 5. A compound according to claim 4 wherein: A is O or CH₂.
 6. A compound according to claim 5 wherein: Q is Q-1.
 7. A compound according to claim 5 wherein: Q is Q-2.
 8. A compound according to claim 5 wherein: Q is Q-3.
 9. A compound according to claim 5 wherein: Q is Q-4.
 10. A compound according to claim 5 wherein: Q is Q-5.
 11. A compound according to claim 5 wherein: Q is Q-8.
 12. A compound according to claim 6 which is: methyl 3,3a,4,5-tetrahydro-2-[[[4-trifluoromethyl)phenyl]-amino]carbonyl]-2H-pyrazolo[3,4-f]-quinoline-3a-carboxylate.
 13. A compound according to claim 9 which is: methyl 3,3a,4,5-tetrahydro-2-[[[4-trifluoromethyl)phenyl]-amino]carbonyl]-2H-pyrazolo[4,3-h]-quinoline-3a-carboxylate.
 14. A compound according to claim 11 which is: methyl 7-fluoro-3A,4-dihydro-2-[[[4-(trifluoromethyl)-phenyl]amino]carbonyl]-3H-pyrazolo[5,1-c]-[1,4]benzoxazine-3a-carboxylate.
 15. A compound according to claim 11 which is: 7-chloro-3A-(4-fluorophenyl)-3A,4-dihydro-N-[4-(trifluoromethyl)phenyl]-3H-pyrazolo[5,1-c][1,4]-benzoxazine-2carboxamide.
 16. An arthropodicidal composition comprising an arthropodically effective amount of a compound according to any one of claims 1-10, 11-13, 14, 15 or 18 a carrier therefor.
 17. A method for controlling arthropods comprising applying to them or their environment an arthropodically effective amount of a compound according to any one of claims 1-10, 13-15, 17, 18 or
 21. 18. A compound according to claim 10 which is: methyl 7-chloro-3,3a,4,5-tetrahydro-N-[[[4-trifluoromethyl)-phenyl]amino]carbonyl]-2H-thieno [2,3-g]-indazole-3a-carboxylate. 